Guanidine Compounds, and Use Thereof as Binding partners for 5-Ht5 Receptors

The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.

5-RING HETEROAROMATIC COMPOUNDS AND THEIR USE AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same. 2. A 5-ring heteroaromatic compound of general formula I according to , and/or corresponding enantiomeric , diastereomeric , and/or tautomeric forms thereof , and/or pharmaceutically acceptable salts thereof , and/or active substance precursors (“prodrugs”) thereof , wherein the radicals W , A , RRRR , B , Rw , D , Q , a b , c , R , R , R , R , V , R , R , R , R , X , Y , Z , unless stated otherwise below , have the same meaning as in , and the radicals below have the following definitions:{'sup': 4', '6, 'R, Rin each case independently stand for a radical selected from groups 1.), 3.), 4.), or 5.), which may be the same or different, and'}{'sup': 5', '7, 'R, Rin each case independently stand for a radical selected from groups 2.), 3.), 4.), or 5.), which may be the same or different,'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein groups 1.)-5.) in each case have the meanings stated in .'}3. A 5-ring heteroaromatic compound of general formula I according to , and/or corresponding enantiomeric , diastereomeric , and/or tautomeric forms thereof , and/or pharmaceutically acceptable salts thereof , and/or active substance precursors (“prodrugs”) thereof , wherein the radicals W , A , R , R , R , R , B , R , D , R , R , R , X , Y , Z , R , R , R , R , R , R , R , R , R , R , R , R , unless stated otherwise below , have the same meaning stated in , and the radicals below have the following definitions:Q: Formula Q1 is the sum of a, b, and c and is equal to 1, 2, or 3;{'sub': Q', 'Q', 'Q', 'Q, 'sup': 1', '2', '3', '4, 'claim-text': {'sub': 1', '6, 'hydrogen, halogen, OH, or optionally substituted C-Calkyl;'}, 'R, R, R, Rindependently stand for{'sub': Q', 'Q', 'Q, 'sup': 5', '5, 'V: is —CO—, —CO—NR—, —NR—CO—, —O—, —S—;'}{'sub': Q', '3, 'sup': '5', 'R: is hydrogen, CH.'}4. A 5-ring ...

Method for producing isocyanates

A process for the preparation of isocyanates from carbamic esters.

Heterocyclic compounds and their use as binding partners for 5-HT5 receptors

The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions.

Hetaryl-substituted guanidine compounds and use thereof as binding partners for 5-HT5-receptors

The invention relates to the hetaryl-substituted guanidine compounds of general formula (I), enantiomeres, diastereomeres and/or tautomeres thereof, in addition to the pharmaceutically acceptable salts thereof and the prodrugs of the known compounds. The invention also relates to the use of said hetaryl-substituted guanidine compounds as binding partners for 5-HT5-receptors for treating and/or for the prophylaxis of illnesses which are modulated by a 5-HT5-receptor activity, in particular, for treating and/or for the prophylaxis of neurodegenerative and neuropsychiatric disorders, and signs, symptoms and dysfunctions associated with said disorders.

Guanidine compounds, and use thereof as binding partners for 5-HT5 receptors

The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.

GUANIDINE COMPOUNDS, AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The present invention relates to guanidine compounds of the general formula I 3. Guanadine compound according to or , wherein the given moieties have the following definition:W: W1;{'sub': 3', '2', '3', '2, 'claim-text': [{'sub': 1', '6', '2', '6, 'each optionally substituted C-C-alkyl or C-C-alkenyl,'}, {'sub': 2', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A, 'sup': 1', '1', '1', '2', '3', '4', '1', '4', '1, 'O—CH—COO—R, O—R, S—R, NRR, NR—CO—Ror CO—NRR;'}], 'A: halogen, OH, CN, CF, CHF, OCF, OCHF, or'}{'sub': A', '1', '4', '3', '7, 'sup': '1', 'R: each optionally substituted C-C-alkyl, C-C-cycloalkyl, phenyl or benzyl;'}{'sub': 'A', 'sup': '2', 'claim-text': {'sub': 1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl or SO—C-C-alkylene-aryl;'}, 'R: hydrogen, or'}{'sub': A', '1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'sup': '3', 'claim-text': {'sub': A', 'A, 'sup': 2', '3, 'or the moieties Rand Rtogether form an optionally substituted 5- or 6-membered saturated or unsaturated ring, which can contain up to two identical or different heteroatoms from the group O and N;'}, 'R: each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl, or SO—C-C-alkylene-aryl;'}{'sub': A', '1', '4, 'sup': '4', 'R: hydrogen or an optionally substituted C-C-alkyl moiety;'}B: hydrogen or as moiety A is defined;{'sub': W', '3', '3, 'sup': '1', 'claim-text': {'sub': 1', '4', '1', '6', '1', '6, 'each optionally substituted C-C-alkyl, aryl, C-C-alkylamino or C-C-dialkylamino;'}, 'R: hydrogen, F, Cl, CN, CF, O—CF, or'}in the formula Z1 the sum of a, b and c is 1, 2 or 3;{'sub': Z', 'Z', 'Z', 'Z, 'sup': 1', '2', '3', '4, 'claim-text': {'sub': 1', '6, 'hydrogen, halogen, OH, optionally substituted C-C-alkyl;'}, 'R, R, R, Rindependently of ...

Substituted isoquinolines and phthalazines as inhibitors of phosphodiesterase type 10A

The present invention relates to novel compounds of the formula (I), wherein Het, A, Q, X1, X2, X3, R1 and R2 are defined in the specification, which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

5-Ring Heteroaromatic compounds and their use as binding partners for 5-ht5 receptors

The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 2. The compound of claim 1 , where Ris selected from the group consisting of halogen claim 1 , CN claim 1 , OH claim 1 , C-C-alkyl claim 1 , fluorinated C-C-alkyl claim 1 , C-C-alkoxy claim 1 , fluorinated C-C-alkoxy claim 1 , C-C-cycloalkyl claim 1 , fluorinated C-C-cycloalkyl claim 1 , N(R)(R) claim 1 , C-C-alkyl-N(R)(R) claim 1 , C(O)O—R claim 1 , C(O)N(R)(R) claim 1 , N(R)S(O)(R) and S(O)N(R)(R).3. The compound of claim 1 , where Xis C—H.4. The compound of claim 1 , where Xis N.5. The compound of claim 1 , where Xis C—R.6. The compound of claim 1 , where Xis N.7. The compound of claim 1 , where Y is O.8. The compound of claim 1 , where Ris C-C-alkyl claim 1 , C-C-cycloalkyl or C-C-cycloalkylmethyl.9. The compound of claim 8 , where Ris a radical of the formula CHRR claim 8 , where Ris selected from the group consisting of hydrogen and C-C-alkyl and where Rb is selected from the group consisting of C-C-alkyl.10. The compound of claim 1 , where Ris a moiety Z—Ar.11. (canceled)12. The compound of claim 1 , where{'sup': 21', '22', 'g', 'h, 'sub': '2', 'Rand Rtogether with the carbon atom, to which they are bound form a saturated 5- to 7-membered carbocyclic ring or a saturated 5- to 7-membered heterocyclic ring which has 1, 2 or 3 heteroatoms or heteroatom containing groups selected from the group of O, N, S, SO and SOas ring members, where the carbocyclic ring and the heterocyclic ring may be unsubstituted or may be substituted by 1, 2 or 3 identical or different substituents R, and where the carbocyclic ring and the heterocyclic ring may carry a fused benzene ring or a fused 5- ...

Tetraline and indane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.

FUSED HETEROCYCLIC COMPOUNDS AS S1P MODULATORS

The invention relates to heterocyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.

Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.

FUSED (HETERO)CYCLIC COMPOUNDS AS S1P MODULATORS

The invention relates to (hetero)cyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.

AMINOINDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.

AMINOINDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to aminoindane derivatives of the formula (I) 2. Compound as claimed in claim 1 , wherein A is a benzene ring.3. Compound as claimed in claim 1 , wherein —Y-A-X— comprises at least 2 claim 1 , 3 or 4 atoms in the main chain.4. Compound as claimed in claim 1 , wherein Ris C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , C-C-cycloalkyl claim 1 , or optionally substituted C-C-heterocyclyl.5. Compound as claimed in claim 1 , wherein Ais a bond.6. Compound as claimed in claim 1 , wherein W is a bond and Y is a bond claim 1 , or W is a bond and Y is —NR—.7. Compound as claimed in claim 1 , wherein Xis —O— and Ais C-C-alkylene claim 1 , or Xis C-C-alkylene and Ais a bond.8. Compound as claimed in claim 1 , wherein R—W-A-Q-Y-A-X— is R—S(O)—NR-A-X— or R—S(O)—X—.10. Compound as claimed in claim 1 , wherein Ris C-C-alkyl claim 1 , C-C-cycloalkyl claim 1 , C-C-alkoxycarbonyl or C-C-heterocyclyl.11. Compound as claimed in claim 1 , wherein Ris hydrogen.12. Compound as claimed in claim 1 , wherein R claim 1 , Rtogether are optionally substituted C-C-alkylene claim 1 , wherein one —CH— of C-C-alkylene may be replaced by an oxygen atom.13. Compound as claimed in claim 1 , wherein Xis CRRand Xis a bond.14. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl claim 1 , or R claim 1 , Rtogether are optionally substituted C-C-alkylene.15. Compound as claimed in claim 1 , wherein Ris optionally substituted aryl.17. Compound as claimed in claim 1 , whereinA is a benzene ring;{'sup': 1', '1', '2', '1, 'R is R—W-A-Q-Y-A-X—;'}{'sup': '1', 'sub': 1', '6', '3', '12', '1', '4', '3', '12', '3', '12, 'Ris C-C-alkyl, C-C-cycloalkyl-C-C-alkyl, C-C-cycloalkyl, or optionally substituted C-C-heterocyclyl;'}W is a bond;{'sup': '1', 'Ais a bond;'}{'sub': '2', 'Q is —S(O)—;'}{'sup': '9', 'Y is —NR— or a bond;'}{'sup': '2', 'sub': 1', '4, 'Ais C-C-alkylene or a bond;'}{'sup': '1', 'sub': 1', '4, 'Xis —O— or C-C-alkylene;'}{' ...

Method for producing prepolymers containing isocyanate groups and urethane groups

The invention relates to a method for producing prepolymers containing isocyanate groups and urethane groups. The inventive method comprises the following steps a) at least one polyisocyanate having a stoichiometric deficit of at least one t compound is reacted with at least two hydrogen atoms reacting with isocyanate groups, and b) the reaction product from step a) is distilled by means of a molecular evaporator.

Inhibitor compounds of phosphodiesterase type 10A

The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein X1is CH or N, X2is C—R5or N, Y is O or S, R1is inter alia C2-C8-alkyl, C2-C8-alkenyl, C1-C4-fluoroalkyl, C3-C8-cycloalkyl, C5-C8-cycloalkyl carrying a fused benzene ring, or a moiety Z1—Ar1; R2is a radical of the formula CR21R22R23or phenyl or 5- or 6-membered hetaryl having 1, 2 or 3 heteroatoms as ring members which are selected from O, S and N, where phenyl and monocyclic hetaryl are unsubstituted or may carry 1, 2 or 3 identical or different substituents Ra, R3is inter alia hydrogen, C1-C8-alkyl, C2-C8-alkenyl, C1-C4-fluoroalkyl, C3-C8-cycloalkyl, etc, or R2and R3together with the nitrogen ...

Heataryl-substituted guanidine compounds and use thereof as binding partners for 5-ht5-receptors

The invention relates to the hetaryl-substituted guanidine compounds of general formula (I), enantiomeres, diastereomeres and/or tautomeres thereof, in addition to the pharmaceutically acceptable salts thereof and the prodrugs of the known compounds. The invention also relates to the use of said hetaryl-substituted guanidine compounds as binding partners for 5-HT5-receptors for treating and/or for the prophylaxis of illnesses which are modulated by a 5-HT5-receptor activity, in particular, for treating and/or for the prophylaxis of neurodegenerative and neuropsychiatric disorders, and signs, symptoms and dysfunctions associated with said disorders.

Aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.

GUANIDINE COMPOUNDS, AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.

Inhibitor compounds of phosphodiesterase type 10A

The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

GUANIDINE COMPOUNDS AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The present invention relates to guanidine compounds of the general formula I 3. Guanadine compound according to or , wherein the given moieties have the following definition:W: W1;{'sub': 3', '2', '3', '2, 'claim-text': {'sub': 1', '6', '2', '6', '2', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A', 'A, 'sup': 1', '1', '1', '2', '3', '4', '1', '4', '1, 'each optionally substituted C-C-alkyl or C-C-alkenyl, O—CH—COO—R, O—R, S—R, NRR, NR—CO—Ror CO—NRR;'}, 'A: halogen, OH, CN, CF, CHF, OCF, OCHF, or'}{'sub': A', '1', '4', '3', '7, 'sup': '1', 'R: each optionally substituted C-C-alkyl, C-C-cycloalkyl, phenyl or benzyl;'}{'sub': 'A', 'sup': '2', 'claim-text': {'sub': 1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl or SO—C-C-alkylene-aryl;'}, 'R: hydrogen, or'}{'sub': A', '1', '4', '1', '4', '1', '4', '2', '1', '4', '2', '2', '2', '1', '4, 'sup': '3', 'claim-text': {'sub': A', 'A, 'sup': 2', '3, 'or the moieties Rand Rtogether form an optionally substituted 5- or 6-membered saturated or unsaturated ring, which can contain up to two identical or different heteroatoms from the group O and N;'}, 'R: each optionally substituted C-C-alkyl, phenyl, benzyl, phenethyl, CO—C-C-alkyl, CO-aryl, CO—O—C-C-alkyl, SO—C-C-alkyl, SO-aryl, SO-hetaryl, or SO—C-C-alkylene-aryl;'}{'sub': A', '1', '4, 'sup': '4', 'R: hydrogen or an optionally substituted C-C-alkyl moiety;'}B: hydrogen or as moiety A is defined;{'sub': w', '3', '3, 'sup': '1', 'claim-text': {'sub': 1', '4', '1', '6', '1', '6, 'each optionally substituted C-C-alkyl, aryl, C-C-alkylamino or C-C-dialkylamino;'}, 'R: hydrogen, F, Cl, CN, CF, O—CF, or'}in the formula Z1 the sum of a, b and c is 1, 2 or 3;{'sub': Z', 'Z', 'Z', 'Z, 'sup': 1', '2', '3', '4, 'claim-text': {'sub': 1', '6, 'hydrogen, halogen, OH, optionally substituted C-C-alkyl;'}, 'R, R, R, Rindependently of one another ...

Substituted furo[3,2-c]pyridines, thieno[3,2-c]pyridines, thieno[2,3-d]pyridazines and pyrido[3,4-d]pyridazines as phosphodiesterase type 10A inhibitors

The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Q is O or S, X1is N or CH, X2is N or C—R7; X3is O, S—X4═C(R8)—, where C(R8) is bound to the carbon atom which carries R2, or —X5═C(R9)—, where X5is bound to the carbon atom which carries R2; X4is N or C—R9; X5is N; Het is selected from optionally substituted phenyl, monocyclic hetaryl and fused bicyclic hetaryl; R1is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkylsulfanyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, the moiety Y1-Cyc1; R2is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl ...

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 3. The compound of claim 1 , where Xis selected from O claim 1 , S claim 1 , —X═C(R)— claim 1 , where C(R) is bound to the carbon atom which carries R.4. The compound of claim 1 , where A is selected from A claim 1 , A claim 1 , Aand A.5. The compound of claim 1 , where Xis C—R.6. The compound of claim 5 , where Ris hydrogen or Y-Cyc.7. The compound of claim 1 , where Xis N.8. The compound of claim 1 , where Xis CH.9. The compound of claim 1 , where Xis S.10. The compound of claim 1 , where Xis O.11. The compound of claim 1 , where Xis C(R)═C(R).12. The compound of claim 1 , where Xis N═(CR).13. The compound of claim 11 , where Ris hydrogen or Y-Cyc.14. The compound of claim 1 , where Xis N═C(R).15. The compound of claim 11 , where Ris hydrogen.16. The compound of claim 1 , where Ris a radical Y-Cyc.17. The compound of claim 1 , where Ris selected from the group consisting of hydrogen claim 1 , fluorine claim 1 , C-C-alkyl claim 1 , C-C-fluoroalkyl claim 1 , C-C-alkoxy claim 1 , C-C-fluoroalkoxy claim 1 , cyclopropyl claim 1 , optionally substituted by 1 claim 1 , 2 or 3 methyl groups claim 1 , and fluorinated cyclopropyl.18. The compound of claim 17 , where Ris hydrogen.19. The compound of claim 1 , where A is A.20. The compound of claim 19 , where R claim 19 , Rare selected from hydrogen and fluorine.21. The compound of claim 19 , where Rand Rare claim 19 , independently of each other claim 19 , selected from the group consisting of hydrogen claim 19 , fluorine and methyl.22. The compound of claim 1 , where A is A.23. The compound of claim 1 , where A is ...

HETEROCYCLIC COMPOUNDS AND THEIR USE AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions.

PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.

Inhibitor compounds of phosphodiesterase type 10A

The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

Substituted pyrazolopyrimidines and method of use

Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, L1and G1are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the γ-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.

Inhibitor compounds of phosphodiesterase type 10A

The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein X1is CH or N, X2is C—R5or N, Y is O or S, R1is inter alia C2-C8-alkyl, C2-C8-alkenyl, C1-C4-fluoroalkyl, C3-C8-cycloalkyl, C5-C8-cycloalkyl carrying a fused benzene ring, or a moiety Z1—Ar1; R2is a radical of the formula CR21R22R23or phenyl or 5- or 6-membered hetaryl having 1, 2 or 3 heteroatoms as ring members which are selected from O, S and N, where phenyl and monocyclic hetaryl are unsubstituted or may carry 1, 2 or 3 identical or different substituents Ra, R3is inter alia hydrogen, C1-C8-alkyl, C2-C8-alkenyl, C1-C4-fluoroalkyl, C3-C8-cycloalkyl, etc, or R2and R3together with the nitrogen ...

Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.

Substituted pyrazolopyrimidines and method of use

Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, L1and G1are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the γ-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.

Inhibitor compounds of phosphodiesterase type 10A

The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

TETRALINE AND INDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to tetraline and indane derivatives of the formula (I) 3. A compound of claim 1 , wherein —Y-A-X— comprises at least 2 claim 1 , 3 or 4 atoms in the main chain.4. A compound of claim 1 , wherein Ris C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , C-C-cycloalkyl claim 1 , or optionally substituted C-C-heterocyclyl.5. A compound of claim 1 , wherein Ais a bond.6. A compound of claim 1 , wherein W is a bond and Y is a bond claim 1 , or W is a bond and Y is —NR—.7. A compound of claim 1 , wherein Xis —O— and Ais C-C-alkylene claim 1 , or Xis C-C-alkylene and Ais a bond.8. A compound of claim 1 , wherein R—W-A-Q-Y-A-X— is R—S(O)—NR-A-X— or R—S(O)—X—.10. A compound of claim 1 , wherein Yis methylene or 1 claim 1 ,2-ethylene.11. A compound of claim 1 , wherein Ris C-C-alkyl claim 1 , C-C-cycloalkyl or C-C-heterocyclyl claim 1 , ore is C-C-alkylene that is bound to a carbon atom in Y.12. A compound of claim 1 , wherein Ris hydrogen or C-C-alkyl.13. A compound of claim 1 , wherein R claim 1 , Rtogether are optionally substituted C-C-alkylene claim 1 , wherein one —CH— of C-C-alkylene may be replaced by an oxygen atom.14. A compound of claim 1 , wherein Xis CRRand Xis a bond.15. A compound of claim 1 , wherein Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl claim 1 , or R claim 1 , Rtogether are optionally substituted C-C-alkylene.17. A compound of claim 1 , whereinA is a benzene ring;{'sup': 1', '1', '2', '1, 'R is R—W-A-Q-Y-A-X—;'}{'sup': '1', 'sub': 1', '6', '3', '12', '1', '4', '3', '12', '3', '12, 'Ris C-C-alkyl, C-C-cycloalkyl-C-C-alkyl, C-C-cycloalkyl, or optionally substituted C-C-heterocyclyl;'}W is a bond;{'sup': '1', 'Ais a bond;'}{'sub': '2', 'Q is —S(O)—;'}{'sup': '9', 'Y is —NR— or a bond;'}{'sup': '2', 'sub': 1', '4, 'Ais C-C-alkylene or a bond;'}{'sup': '1', 'sub': 1', '4, 'Xis —O— or C-C-alkylene;'}{'sup': '2', 'Ris hydrogen or halogen;'}{'sup': '3', 'Ris hydrogen;'}{'sup': '1', 'sub': 1', '4, 'Yis optionally ...

Guanidine compounds, and use thereof as binding partners for 5-HT5 receptors

The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.

Isoindoline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to isoindoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such isoindoline derivatives, and the use of such isoindoline derivatives for therapeutic purposes.

Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to phenalkylamine derivatives of the formula (I) or (II) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.

Guanidine compounds, and use thereof as binding partners for 5-HT5 receptors

The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.

Inhibitor compounds of phosphodiesterase type 10A

The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables X1 is CH or N, X2 is O or S and where R1, R2, R3, R4 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

TETRALINE AND INDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 2. The compound of claim 1 , where Xis N claim 1 , Xis C—R claim 1 , Xis C—Rand Xis C—R.3. The compound of claim 1 , where Xis C—R claim 1 , Xis C—R claim 1 , Xis C—Rand Xis C—R.4. The compound of claim 1 , where either Ror Ris a radical Y-Cyc and Rand R claim 1 , if present claim 1 , have a meaning different from Y-Cyc.5. The compound of claim 4 , where Xis C—Rand Ris a radical Y-Cyc.6. The compound of claim 5 , where Xis N or C—R claim 5 , Xis C—Rand Xis C—R.7. The compound of claim 5 , where R claim 5 , Rand R claim 5 , if present claim 5 , are selected claim 5 , independently of each other claim 5 , from the group consisting of hydrogen claim 5 , fluorine claim 5 , C-C-alkyl claim 5 , C-C-fluoroalkyl claim 5 , C-C-alkoxy claim 5 , C-C-fluoroalkoxy claim 5 , cyclopropyl claim 5 , optionally substituted by 1 claim 5 , 2 or 3 methyl groups claim 5 , and fluorinated cyclopropyl.8. The compound of claim 4 , where Xis C—Rand Ris a radical Y-Cyc.9. The compound of claim 8 , where Xis C—R claim 8 , Xis C—Rand Xis C—R.10. The compound of claim 8 , where R claim 8 , Rand R claim 8 , if present claim 8 , are selected claim 8 , independently of each other claim 8 , from the group consisting of hydrogen claim 8 , fluorine claim 8 , C-C-alkyl claim 8 , C-C-fluoroalkyl claim 8 , C-C-alkoxy claim 8 , C-C-fluoroalkoxy claim 8 , cyclopropyl claim 8 , optionally substituted by 1 claim 8 , 2 or 3 methyl groups claim 8 , and fluorinated cyclopropyl.11. The compound of claim 1 , where A is a radical CRR.13. The compound of claim 12 , where Ris a radical Y-Cyc ...

PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to phenalkylamine derivatives of the formula (I) or (II) 2. Compound as claimed in claim 1 , wherein —Y-A- comprises at least 1 or 2 atoms in the main chain.3. Compound as claimed in claim 1 , wherein Ris C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , halogenated C-C-alkyl claim 1 , C-C-alkoxy-C-C-alkyl claim 1 , amino-C-C-alkyl claim 1 , C-C-alkylamino-C-C-alkyl claim 1 , di-C-C-alkylamino-C-C-alkyl claim 1 , C-C-alkyloxycarbonylamino-C-C-alkyl claim 1 , C-C-alkylaminocarbonylamino-C-C-alkyl claim 1 , C-C-aryl-C-C-alkyl claim 1 , C-C-cycloalkyl claim 1 , C-C-alkenyl claim 1 , optionally substituted C-C-aryl claim 1 , hydroxy claim 1 , C-C-alkylamino claim 1 , (halogenated C-C-alkyl)amino claim 1 , di-C-C-alkylamino or optionally substituted C-C-heterocyclyl.5. Compound as claimed in claim 1 , wherein R—W-A-Q-Y-Ais R—S(O)—NH-A claim 1 , R—NH—S(O)-A claim 1 , R—C(O)—NH-A- or R—NH—C(O)-A-.6. Compound as claimed in claim 1 , wherein n is 1.7. Compound as claimed in claim 1 , wherein Xis —O— or —NR—.9. Compound as claimed in claim 1 , wherein R—W-A-Q- is R—S(O)—NH— claim 1 , R—NH—S(O)— claim 1 , R—C(O)—NH— or R—NH—C(O)—.10. Compound as claimed in claim 1 , wherein m is 1 or 2.11. Compound as claimed in claim 1 , wherein Xis CRR claim 1 , and Xis a bond.12. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl claim 1 , or R claim 1 , Rtogether are optionally substituted C-C-alkylene.14. Compound as claimed in claim 1 , wherein Yis a bond and Yis >CRR claim 1 ,15. Compound as claimed in claim 1 , wherein Ra is hydrogen claim 1 , C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , halogenated C-C-alkyl claim 1 , amino-C-C-alkyl claim 1 , CHCN claim 1 , C-C-aryl-C-C-alkyl claim 1 , —CHO claim 1 , C-C-alkylcarbonyl claim 1 , (halogenated C-C-alkyl)carbonyl claim 1 , C-C-arylcarbonyl claim 1 , C-C-cycloalkyl claim 1 , C-C-alkoxycarbonyl claim 1 , C-C-aryloxycarbonyl claim 1 , —C(═NH)NH claim ...

TETRAHYDROISOQUINOLINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.

Benzazepine derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to benzazepine derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such benzazepine derivatives, and the use of such benzazepine derivatives for therapeutic purposes.

AMINOTETRALINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to aminotetraline derivatives of the formula (I) 234.-. (canceled)35. A method for inhibiting the glycine transporter GlyT1 in a mammal in need thereof which comprises the administration of an effective amount of a compound of .36. (canceled)37. A method for treating a neurologic or psychiatric disorder or pain in a mammalian patient in need thereof which comprises administering to the patient a therapeutically effective amount of a compound of .38. (canceled)39. The compound of for use in a method of treating a neurologic or psychiatric disorder or pain.40. The method as claimed in claim 37 , wherein the disorder is associated with glycinergic or glutamatergic neurotransmission dysfunction.41. The method as claimed in claim 37 , wherein the neurologic disorder is selected from the group consisting of dementia claim 37 , cognitive impairment claim 37 , and attention deficit disorder.42. The method as claimed in claim 41 , wherein the attention deficit disorder is an attention deficit disorder with hyperactivity.43. The method as claimed in claim 37 , wherein the psychiatric disorder is selected from the group consisting of anxiety disorder claim 37 , depression claim 37 , bipolar disorder claim 37 , schizophrenia claim 37 , and psychosis.44. (canceled) This claims the benefit of U.S. Provisional Application No. 61/152,825, which was filed on Feb. 16, 2009, the contents of which are incorporated herein by reference.The present invention relates to aminotetraline derivatives, pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.Dysfunction of glutamatergic pathways has been implicated in a number of disease states in the human central nervous system (CNS) including but not limited to schizophrenia, cognitive deficits, dementia, Parkinson disease, Alzheimer disease and bipolar disorder. A large ...

PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to phenalkylamine derivatives of the formula (I) or (II) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.

Tetrahydroisoquinolines, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.

Fused (hetero)cyclic compounds as S1P modulators

The invention relates to (hetero)cyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 2. The compound of claim 1 , where Ris selected from the group consisting of halogen claim 1 , CN claim 1 , OH claim 1 , C-C-alkyl claim 1 , fluorinated C-C-alkyl claim 1 , C-C-alkoxy claim 1 , fluorinated C-C-alkoxy claim 1 , C-C-cycloalkyl claim 1 , fluorinated C-C-cycloalkyl claim 1 , N(R)(R) claim 1 , C-C-alkyl-N(R)(R) claim 1 , C(O)O—R claim 1 , C(O)N(R)(R) claim 1 , N(R)S(O)(R) and S(O)N(R)(R).3. The compound of claim 1 , where Xis C—H.4. The compound of claim 1 , where Xis N.5. The compound of claim 1 , where Xis C—R.6. The compound of claim 1 , where Xis N.7. The compound of claim 1 , where Y is O.8. The compound of claim 1 , where Ris C-C-alkyl claim 1 , C-C-cycloalkyl or C-C-cycloalkylmethyl.9. The compound of claim 8 , where Ris a radical of the formula CHRR claim 8 , where Ris selected from the group consisting of hydrogen and C-C-alkyl and where Ris selected from the group consisting of C-C-alkyl.10. The compound of claim 1 , where Ris a moiety Z—Ar.11. The compound of claim 1 , where Ris a radical of the formula CRRR.12. The compound of claim 11 , where{'sup': 21', '22', 'g', 'h', 'h', 'g, 'sub': '2', 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'Rand Rtogether with the carbon atom, to which they are bound form a saturated 5- to 7-membered carbocyclic ring or a saturated 5- to 7-membered heterocyclic ring which has 1, 2 or 3 heteroatoms or heteroatom containing groups selected from the group of O, N, S, SO and SOas ring members, where the carbocyclic ring and the heterocyclic ring may be unsubstituted or may be substituted by 1, 2 or 3 identical or different ...

5-ring heteroaromatic compounds and their use as binding partners for 5-HT5 receptors

The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.

AMINOTETRALINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to aminotetraline derivatives of the formula (I) 4. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , halogen or C-C-alkoxy.6. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl.8. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , halogenated C-C-alkyl claim 1 , amino-C-C-alkyl claim 1 , CHCN claim 1 , —CHO claim 1 , C-C-alkylcarbonyl claim 1 , (halogenated C-C-alkyl)carbonyl claim 1 , C-C-arylcarbonyl claim 1 , C-C-alkoxycarbonyl claim 1 , C-C-aryloxycarbonyl claim 1 , —C(═NH)NH claim 1 , —C(═NH)NHCN claim 1 , C-C-alkylsulfonyl claim 1 , amino claim 1 , —NO or C-C-heterocyclyl.9. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl.10. Compound as claimed in claim 1 , wherein R claim 1 , Rtogether are optionally substituted C-C-alkylene claim 1 , wherein one —CH— of C-C-alkylene may be replaced by an oxygen atom.11. Compound as claimed in claim 1 , wherein Xis CRR.12. Compound as claimed in claim 11 , wherein Xis a bond.13. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl.14. Compound as claimed in claim 1 , wherein R claim 1 , Rtogether are optionally substituted C-C-alkylene.15. Compound as claimed in claim 1 , wherein Ris optionally substituted aryl or optionally substituted C-C-cycloalkyl.17. Compound as claimed in claim 1 , wherein n is 1.18. Compound as claimed in claim 1 , which is:7-Amino-8-(3,4-dichlorobenzyl)-5,6,7,8-tetrahydronaphthalene-2-carbonitrile;7-Amino-8-(4-chlorobenzyl)-5,6,7,8-tetrahydronaphthalene-2-carbonitrile;Ethyl [7-cyano-1-(3,4-dichlorobenzyl)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamate;tert-Butyl [7-cyano-1-(3,4-dichlorobenzyl)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamate,or a physiologically tolerated salt thereof.19. A pharmaceutical composition comprising a carrier and a compound of .20. A method for treating a neurologic or psychiatric disorder ...

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 2. The compound of claim 1 , where Ris selected from the group consisting of halogen claim 1 , CN claim 1 , OH claim 1 , C-C-alkyl claim 1 , fluorinated C-C-alkyl claim 1 , C-C-alkoxy claim 1 , fluorinated C-C-alkoxy claim 1 , C-C-cycloalkyl claim 1 , fluorinated C-C-cycloalkyl claim 1 , N(R)(R) claim 1 , C-C-alkyl-N(R)(R) claim 1 , C(O)O—R claim 1 , C(O)N(R)(R) claim 1 , N(R)S(O)(R) and S(O)N(R)(R).3. The compound of claim 1 , where Xis C—H.4. The compound of claim 1 , where Xis N.5. The compound of claim 1 , where Xis C—R.6. The compound of claim 1 , where Xis N.7. The compound of claim 1 , where Y is O.8. The compound of claim 1 , where Ris C-C-alkyl claim 1 , C-C-cycloalkyl or C-C-cycloalkylmethyl.9. The compound of claim 8 , where Ris a radical of the formula CHRR claim 8 , where Ris selected from the group consisting of hydrogen and C-C-alkyl and where Ris selected from the group consisting of C-C-alkyl.10. The compound of claim 1 , where Ris a moiety Z—Ar.11. The compound of claim 1 , where Ris a radical of the formula CRRR.12. The compound of claim 11 , where{'sup': 21', '22', 'g', 'h', 'h', 'g, 'sub': '2', 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'Rand Rtogether with the carbon atom, to which they are bound form a saturated 5- to 7-membered carbocyclic ring or a saturated 5- to 7-membered heterocyclic ring which has 1, 2 or 3 heteroatoms or heteroatom containing groups selected from the group of O, N, S, SO and SOas ring members, where the carbocyclic ring and the heterocyclic ring may be unsubstituted or may be substituted by 1, 2 or 3 identical or different ...

SPIRO-CYCLIC AMINE DERIVATIVES AS S1P MODULATORS

The present invention is directed to spiro-cyclic amine derivatives which are modulators of S1P receptors and are useful in the treatment of CNS disorders. 4. The compound of claim 1 , which is a hydrochloric acid salt.5. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and at least one pharmaceutically acceptable carrier.6. A method of modulating S1P receptor activity claim 1 , said method comprising contacting a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , with an S1P receptor.7. The method of claim 6 , wherein the S1P is S1P5.8. The method of claim 6 , wherein the contacting comprises administering the compound to a patient.9. A method of treating a disease or disorder associated with S1P5 claim 1 , said method comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.10. A method of treating a CNS disorder in a patient in need thereof claim 1 , said method comprising administering to the patient a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.11. The method of claim 10 , wherein the CNS disorder is Alzheimer's disease claim 10 , or vascular dementia.12. The method of claim 10 , wherein the CNS disorder is Niemann-Pick disease.13. The method of claim 10 , wherein the CNS disorder is Niemann-Pick type C disease.14. The method of claim 10 , wherein the CNS disorder is cognitive deficits in schizophrenia claim 10 , obsessive-compulsive behavior claim 10 , major depression claim 10 , autism claim 10 , multiple sclerosis claim 10 , or pain.15. The method of claim 10 , wherein the CNS disorder is a cognitive disorder.16. The method of claim 15 , wherein the cognitive disorder is age-related cognitive decline.22. A compound claim 17 , which is Compound 1 claim 17 , prepared by the process of . This ...

Fused heterocyclic compounds as S1P modulators

The invention relates to heterocyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.

4-benzylaminoquinolines, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to 4-benzylaminoquinolines of the formula (I) or physiologically tolerated salts thereof. The invention relates to pharmaceutical compositions comprising such quinolines, and the use of such quinolines for therapeutic purposes. The quinolines are GIyTI inhibitors.

EXTRACORPOREAL BLOOD TREATMENT MACHINE COMPRISING A POKA-YOKE FOR A PRESSURE SENSOR

An extracorporeal blood treatment machine includes a blood treatment device, a conveying device for conveying blood through the blood treatment device, and a connection mask designed to interchangeably receive a tube set in a predefined arrangement. The tube set has pressure-monitoring lines that branch off from the tube set and can be connected to pressure sensor connections located on the connection mask. The pressure sensor connections are spaced apart and positioned so as to match the tube set such that, when the tube set is mounted in the predefined arrangement on the connection mask, each pressure-monitoring line, owing to its limited length and the predefined arrangement of the associated branch on the blood treatment machine, can be connected exclusively to only one of the pressure sensor connections. A corresponding tube set is used with the extracorporeal blood treatment machine.

Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.

Heterocyclic compounds, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to heterocyclic compounds of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such heterocyclic compounds, and the use of such heterocyclic compounds for therapeutic purposes.

Substituted isoxazolopyridazinones and isothiazolopyridazinones and methods of use

Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2and R3are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the γ-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.

Heterocyclic compounds, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to heterocyclic compounds of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such heterocyclic compounds, and the use of such heterocyclic compounds for therapeutic purposes.

Inhibitor compounds of phosphodiesterase type 10A

The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. where in formula I the variables X, Y, Q1, Q2 have the following meanings: X is CR3 or N; Q1 is S or O and Q2 is CR4 or N and Q2 is connected to X via a double bond while Q1 is connected to X via a single bond; or Q2 is S or O and Q1 is CR4 or N and Q1 is connected to X via a double bond while Q2 is connected to X via a single bond; Y is CR5 or N; where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders ...

Tetraline and indane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.

Inhibitor compounds of phosphodiesterase type 10A

The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

Tetrahydroisoquinolines, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to tetrahydroisoquinoline of the formula (I) 3. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , halogen or C-C-alkoxy.5. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl.6. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , C-C-alkyl claim 1 , halogenated C-C-alkyl claim 1 , amino-C-C-alkyl claim 1 , CHCN claim 1 , C-C-alkylcarbonyl claim 1 , (halogenated C-C-alkyl)carbonyl claim 1 , —C(═NH)NH claim 1 , —C(═NH)NHCN claim 1 , C-C-alkylsulfonyl claim 1 , amino claim 1 , —NO or C-C-heterocyclyl.7. Compound as claimed in claim 1 , wherein Ris C-C-alkyl and Ris hydrogen or C-C-alkyl claim 1 , or wherein R claim 1 , Rtogether are optionally substituted C-C-alkylene.8. Compound as claimed in claim 1 , wherein Ris optionally substituted C-C-aryl.10. Compound as claimed in claim 1 , wherein Ris optionally substituted C-C-heterocyclyl.12. Compound as claimed in claim 1 , which is:1-[1-(4-Chlorophenyl)cyclobutyl]-1,2,3,4-tetrahydroisoquinoline-7-carbonitrile;1-[2-(4-Chlorophenyl)propan-2-yl]-1,2,3,4-tetrahydroisoquinoline-7-carbonitrile; and1-[1-(Pyridin-2-yl)cyclobutyl]-1,2,3,4-tetrahydroisoquinoline-7-carbonitrile.13. Pharmaceutical composition which comprises a carrier and a compound of .14. A method for treating a neurologic or psychiatric disorder in a mammalian patient in need thereof which comprises administering to the patient a therapeutically effective amount of a compound of claim 1 , wherein the neurologic disorder is selected from the group consisting of dementia claim 1 , cognitive impairment claim 1 , and attention deficit disorder claim 1 , and wherein the psychiatric disorder is selected from the group consisting of anxiety disorder claim 1 , depression claim 1 , bipolar disorder claim 1 , schizophrenia claim 1 , and psychosis. This application is a divisional of U.S. application Ser. No. 12/933,326 filed on Dec. 20, 2010 which is the U.S. National Stage of International Patent ...

BENZAZEPINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to benzazepine derivatives of the formula (I) 2. The compound of claim 1 , wherein R is R—W-A-Q-Y-A-X— and —Y-A-X— comprises at least 2 claim 1 , 3 or 4 atoms in the main chain.3. (canceled)4. The compound of claim 1 , wherein Ris C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , C-C-cycloalkyl claim 1 , or optionally substituted C-C-heterocyclyl.5. The compound of claim 1 , wherein Ais a bond claim 1 , W is a bond and Y is —NR—.67.-. (canceled)8. The compound of claim 1 , wherein Xis —O— and Ais C-C-alkylene claim 1 , or Xis C-C-alkylene and Ais a bond.9. The compound of claim 1 , wherein R—W-A-Q-Y-AX— is R—S(O)—NR-A-X— or R—S(O)—X—.11. The compound of claim 1 , wherein Ris hydrogen or halogen.13. The compound of claim 1 , wherein Ais —CH— claim 1 , —O— claim 1 , or —S—.14. The compound of claim 1 , wherein Ris hydrogen.15. The compound of claim 1 , wherein Ris hydrogen claim 1 , C-C-alkyl claim 1 , or C-C-cycloalkyl.16. The compound of claim 1 , wherein Xis cRRand Xis a bond.17. (canceled)18. The compound of claim 1 , wherein Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl claim 1 , or R claim 1 , Rtogether are optionally substituted C-C-alkylene.1920.-. (canceled)2223-. (canceled)24. The compound of claim 1 , wherein{'sup': 1', '1', '2', '1, 'R is R—W-A-Q-Y-A-X—;'}{'sup': '1', 'sub': 1', '6', '3', '12', '1', '4', '3', '12', '3', '12, 'Ris C-C-alkyl, C-C-cycloalkyl-C-C-alkyl, C-C-cycloalkyl, or optionally substituted C-C-heterocyclyl;'}W is a bond;{'sup': '1', 'Ais a bond;'}{'sub': '2', 'Q is —S(O)—;'}{'sup': '9', 'Y is —NR— or a bond;'}{'sup': '2', 'sub': 1', '4, 'Ais C-C-alkylene;'}{'sup': '1', 'sub': 1', '4, 'Xis —O— or C-C-alkylene;'}{'sup': '2', 'Ris hydrogen or halogen;'}{'sup': 3', '16, 'sub': '2', 'Ais —CH—, —O—, —NR, or —S—;'}{'sup': '3', 'Ris hydrogen;'}{'sup': '4', 'sub': 1', '6', '3', '12', '3', '12', '1', '4, 'Ris hydrogen, C-C-alkyl, C-C-cycloalkyl or C-C-cycloalkyl-C-C-alkyl;'}{'sup': '3', 'Xis a bond;'}{' ...

Inhibitor compounds of phosphodiesterase type 10A

The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

Aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.

4-BENZYLAMINOQUINOLINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to 4-benzylaminoquinolines of the formula (I) or physiologically tolerated salts thereof. The invention relates to pharmaceutical compositions comprising such quinolines, and the use of such quinolines for therapeutic purposes. The quinolines are GIyTI inhibitors.

Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.

Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 3. The compound of claim 1 , where Xis selected from O claim 1 , S claim 1 , —X═C(R)— claim 1 , where C(R) is bound to the carbon atom which carries R.4. The compound of claim 1 , where A is selected from A claim 1 , A claim 1 , Aand A.5. The compound of claim 1 , where Xis C—R.6. The compound of claim 5 , where Ris hydrogen or Y-Cyc.7. The compound of claim 1 , where Xis N.8. The compound of claim 1 , where Xis CH.9. The compound of claim 1 , where Xis S.10. The compound of claim 1 , where Xis O.11. The compound of claim 1 , where Xis C(R)═C(R).12. The compound of claim 1 , where Xis N═(CR).13. The compound of claim 11 , where Ris hydrogen or Y-Cyc3.14. The compound of claim 1 , where Xis N═C(R).15. The compound of claim 11 , where Ris hydrogen.16. The compound of claim 1 , where Ris a radical Y-Cyc.17. The compound of claim 1 , where Ris selected from the group consisting of hydrogen claim 1 , fluorine claim 1 , C-C-alkyl claim 1 , C-C-fluoroalkyl claim 1 , C-C-alkoxy claim 1 , C-C-fluoroalkoxy claim 1 , cyclopropyl claim 1 , optionally substituted by 1 claim 1 , 2 or 3 methyl groups claim 1 , and fluorinated cyclopropyl.18. The compound of claim 17 , where Ris hydrogen.19. The compound of claim 1 , where A is A.20. The compound of claim 19 , where R claim 19 , Rare selected from hydrogen and fluorine.21. The compound of claim 19 , where Rand Rare claim 19 , independently of each other claim 19 , selected from the group consisting of hydrogen claim 19 , fluorine and methyl.22. The compound of claim 1 , where A is A.23. The compound of claim 1 , where A is ...

ISOINDOLINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to isoindoline derivatives of the formula (I) 2. Compound as claimed in claim 1 , wherein R is R—W-A-Q-Y-A-X—.3. Compound as claimed in claim 1 , wherein —Y-A-X— comprises at least 2 claim 1 , 3 or 4 atoms in the main chain.4. Compound as claimed in claim 1 , wherein Ris C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , C-C-cycloalkyl claim 1 , or optionally substituted C-C-heterocyclyl.5. Compound as claimed in claim 1 , wherein Ais a bond.6. Compound as claimed in claim 1 , wherein W is a bond and Y is a bond claim 1 , or wherein W is a bond and Y is —NR—.7. (canceled)8. Compound as claimed in claim 1 , wherein Xis —O— and Ais C-C-alkylene claim 1 , or Xis C-C-alkylene and Ais a bond.9. Compound as claimed in claim 1 , wherein R—W-A-Q-Y-A-X— is R—S(O)—NR-A-X— or R—S(O)—X—.11. Compound as claimed in claim 1 , wherein Ris hydrogen or halogen.12. (canceled)13. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl claim 1 , or two radicals Rtogether with the carbon atom to which they are attached form a carbonyl group.14. Compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , C-C-alkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , halogenated C-C-alkyl claim 1 , C-C-cycloalkyl claim 1 , (halogenated C-C-alkyl)carbonyl claim 1 , or C-C-heterocyclyl.15. Compound as claimed in claim 1 , wherein Xis CRRand Xis a bond.16. (canceled)17. Compound as claimed in claim 1 , wherein Ris hydrogen or C-C-alkyl and Ris hydrogen or C-C-alkyl claim 1 , or wherein R claim 1 , Rtogether are optionally substituted C-C-alkylene.18. (canceled)19. (canceled)21. (canceled)22. (canceled)23. Compound as claimed in claim 1 , wherein{'sup': 1', '1', '2', '1, 'R is R—W-A-Q-Y-A-X—;'}{'sup': '1', 'sub': 1', '6', '3', '12', '1', '4', '3', '12', '3', '12, 'Ris C-C-alkyl, C-C-cycloalkyl-C-C-alkyl, C-C-cycloalkyl, or optionally substituted C-C-heterocyclyl;'}W is a bond;{'sup': '1', 'Ais a bond;'}{'sub': '2', 'Q is —S(O)—;'}{'sup': '9', 'Y is —NR— ...

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof 2. The compound of claim 1 , where X is C—R.3. The compound of claim 2 , where Ris hydrogen claim 2 , halogen claim 2 , methyl claim 2 , methoxy claim 2 , CHF claim 2 , CF claim 2 , OCHFor OCF claim 2 , in particular hydrogen.4. The compound of claim 1 , where X is N.5. The compound of any of the preceding claims claim 1 , where Y is N.6. The compound of any of the preceding claims claim 1 , where Ris a radical CN claim 1 , R claim 1 , a moiety Y—NRRor a moiety Z—Ar.7. The compound of claim 6 , where Ris a moiety Z—Ar claim 6 , where Zis a single bond.8. The compound of any of or claim 6 , where Ris a moiety Z—Ar claim 6 , where Aris selected from the group consisting of phenyl claim 6 , thienyl claim 6 , pyrazolyl claim 6 , isoxazolyl claim 6 , thiazolyl and pyridyl claim 6 , where phenyl claim 6 , thienyl claim 6 , pyrazolyl claim 6 , isoxazolyl claim 6 , thiazolyl claim 6 , 1 claim 6 ,2 claim 6 ,4-oxadiazolyl and pyridyl are unsubstituted or carry 1 claim 6 , 2 claim 6 , 3 or 4 identical or different substituents R.9. The compound of any of the preceding claims claim 6 , where Ris a radical R claim 6 , in particular a radical selected from the group consisting of trimethylsilyl claim 6 , C-C-alkyl claim 6 , C-C-cycloalkyl and C-C-cycloalkyl-C-C--alkyl claim 6 , where the three last mentioned radicals may be unsubstituted claim 6 , partially or completely halogenated or where the C-C-cycloalkyl radicals may carry 1 claim 6 , 2 or 3 radicals methyl groups and where Ris especially methyl.10. The compound of any of the preceding claims claim 6 , where one or two of the radicals R claim 6 , R claim 6 , Rand Rare different from hydrogen.11. The compound of claim 10 , where Ris different from hydrogen and one of Rand Ris different from hydrogen.12. The compound of any of the preceding claims claim 10 , where Ris selected ...

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: 2. The compound of claim 1 , where A is C(R claim 1 ,R).3. The compound of claim 2 , where A is CH.4. The compound of any of the preceding claims claim 2 , where X is C(O).5. The compound of claim 4 , where Y is C(R claim 4 ,R).6. The compound of claim 4 , where Rand R claim 4 , independently of each other claim 4 , are selected from the group consisting of hydrogen claim 4 , fluorine and methyl and where Rand Rare especially hydrogen.7. The compound of any of to claim 4 , where Y is C(O).8. The compound of any of the preceding claims claim 4 , where Z is a bond.10. The compound of any one of the preceding claims claim 1 , where Ris selected from the group consisting of saturated 4- claim 1 , 5- claim 1 , 6- claim 1 , 7- or 8-membered heteromonocycles and saturated 7- claim 1 , 8- claim 1 , 9- or 10-membered heterobicycles claim 1 , where the heteromonocycles and the heterobicycles have one nitrogen or oxygen atom as ring member and may have one further heteroatom or heteroatom containing group as ring member claim 1 , which is selected from the group consisting of O claim 1 , S claim 1 , S(═O) claim 1 , S(═O)and N claim 1 , where the saturated heteromonocycle and the saturated heterobicycle are unsubstituted or carry 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 radicals Ror one radical Y′—Rand 0 claim 1 , 1 claim 1 , 2 claim 1 , 3 or 4 radicals R claim 1 , where R claim 1 , Rand Y′ are as defined in .11. The compound of claim 10 , where Z—Ris selected from the group consisting of 1-piperidinyl claim 10 , 4 claim 10 ,4-difluoro-1-piperidinyl claim 10 , 4-hydroxylpiperidin-1-yl claim 10 , 4-piperidinyl claim 10 , 1-methyl-4-piperidinyl claim 10 , 1-piperazinyl claim 10 , 4-methyl-1-piperazinyl claim 10 , 4-(tert.-butyloxycarbonyl)piperazin-1-yl claim 10 , 1-piperazinylmethyl claim 10 , 4-methyl-1-piperazinylmethyl claim ...

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. 2. The compound of claim 1 , where Ris a radical Ror a moiety Z—Ar.3. The compound of claim 1 , where Ris a moiety Z—Ar claim 1 , where Zis a single bond.4. The compound of claim 1 , where Ris a moiety Z—Ar claim 1 , where Aris selected from the group consisting of phenyl claim 1 , thienyl claim 1 , pyrazolyl claim 1 , isoxazolyl claim 1 , thialzolyl claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazolyl and pyridyl claim 1 , where phenyl claim 1 , thienyl claim 1 , pyrazolyl claim 1 , isoxazolyl claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazolyl claim 1 , thialzolyl and pyridyl are unsubstituted or carry 1 claim 1 , 2 claim 1 , 3 or 4 identical or different substituents R.5. The compound of claim 1 , where Ris a radical R claim 1 , in particular a radical selected from the group consisting of trimethylsilyl claim 1 , C-C-alkyl claim 1 , C-C-cycloalkyl and C-C-cycloalkyl-C-C--alkyl claim 1 , where the three last mentioned radicals may be unsubstituted claim 1 , partially or completely halogenated or where the C-C-cycloalkyl radicals may carry 1 claim 1 , 2 or 3 radicals methyl groups and where Ris especially methyl.6. The compound of claim 1 , where Qis N and X is C—R.7. The compound of claim 6 , where Ris selected from the group consisting of hydrogen claim 6 , halogen claim 6 , R claim 6 , OR claim 6 , C-C-alkyl claim 6 , and C-C-alkoxy.8. The compound of claim 6 , where Ris a group Z—Ar.9. The compound of claim 1 , where Qis C—Rand X is N.10. The compound of claim 9 , where Ris selected from the group consisting of hydrogen claim 9 , halogen claim 9 , methoxy claim 9 , methyl claim 9 , and ethyl.11. The compound of claim 6 , where Qis S.12. The compound of claim 6 , where Qis O.13. The compound of claim 1 , where Qis N and X is C—R.14. The compound of claim 13 , where Ris selected from the group consisting of hydrogen claim 13 , ...

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 2. The compound of claim 1 , where both Yand Yin Hetare carbon atoms.3. The compound of claim 1 , where Hetis a bivalent monocyclic 5-membered heteroaromatic radical claim 1 , having 1 heteroatom or heteroatom moiety selected from O claim 1 , S and N—Ras ring member claim 1 , and 0 claim 1 , 1 or 2 further nitrogen atoms as ring members.4. The compound of claim 3 , where Hetis selected from the group consisting of 1-(R)-1H-pyrazole-3 claim 3 ,4-diyl claim 3 , 1-(R)-1H-pyrazole-4 claim 3 ,5-diyl claim 3 , 1H-pyrazole-1 claim 3 ,5-diyl claim 3 , 1-(R)-1H-imidazol-4 claim 3 ,5-diyl claim 3 , isoxazol-4 claim 3 ,5-diyl claim 3 , isoxazol-3 claim 3 ,4-diyl claim 3 , 1-(R)-1H-1 claim 3 ,2 claim 3 ,3-triazol-4 claim 3 ,5-diyl claim 3 , 1H-oxazol-4 claim 3 ,5-diyl claim 3 , 1H-imidazol-1 claim 3 ,2-diyl claim 3 , 1H-imidazol-1 claim 3 ,5-diyl and 1H-1 claim 3 ,3 claim 3 ,4-triazol-1 claim 3 ,2-diyl and where k is 0 or 1.5. The compound of claim 1 , where k in formula I is 0.7. The compound of claim 6 , where Het1/2 is a radical Het1/2a.8. The compound of claim 6 , where Rin radicals Het1/2a to Het1/2q is hydrogen.10. The compound of claim 9 , where Xis C—R claim 9 , Xis C—R claim 9 , Xis C—Rand Xis C—R claim 9 , where R claim 9 , R claim 9 , R claim 9 , R claim 9 , independently of each other claim 9 , are hydrogen or have one of the meanings given for R claim 9 , and where in particular at least 3 of R claim 9 , R claim 9 , Rand Rare hydrogen and at most one of R claim 9 , R claim 9 , Rand Ris a radical R.11. The compound of claim 9 , where each X ...

SPIRO-COMPOUNDS AS SIP MODULATORS

The invention relates to heterocyclic compounds of formula (I) as SIP modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment or alleviation of diseases or disorders mediated by an SIP receptor. 2. A compound according to wherein m and n are both 0 or both 1.4. A compound according to wherein R1 is selected from the group consisting of -1 claim 3 ,3-cyclobutylene-R2 and —(C1-3)alkylene-R2 claim 3 , wherein the (C1)alkyl is unsubstituted claim 3 , and the (C2)alkyl and the (C3)alkyl are substituted with up to two CHgroups claim 3 , with (CH)to form a cyclopropyl moiety or with (CH)to form a cyclobutyl moiety.5. A compound according to wherein X is CH.6. A compound according to wherein R3 is selected from the group consisting of:(C3-6)cycloalkyl, preferably cyclohexyl, optionally substituted with (C1-4) alkyl; halogen,', 'cyano,', '(C1-4)alkyl optionally substituted with one or more fluoro atoms,', '(C1-4)alkoxy optionally substituted with one or more fluoro atoms or with (C3-6)cycloalkyl,', '(C3-5)cycloalkoxy optionally substituted with one or more fluoro atoms; and', '(C3-6)cycloalkyl optionally substituted with (C1-4)alkyl, (C1-4)alkoxy or a halogen atom,, 'monocyclic heterocycle, preferably oxanyl or pyridyl, optionally substituted with 1 or 2 substituents independently selected from the group consisting ofindanyl, optionally substituted with one or two halogen atoms8-10 membered fused bicyclic group, preferably preferably 2,3-dihydrobenzofuranyl, indanyl, indoly or 1,3-dioxaindanyl, optionally substituted with one or two halogen atoms; halogen,', 'cyano,', '(C1-4)alkyl optionally substituted with one or more fluoro atoms,', '(C1-4)alkoxy optionally substituted with one or more fluoro atoms or with (C3-6)cycloalkyl,', '(C3-5)cycloalkoxy optionally substituted with one or more fluoro atoms; and', '(C3-6)cycloalkyl optionally substituted with (C1-4)alkyl, (C1-4)alkoxy or a halogen atom., 'phenyl optionally substituted ...

Novel inhibitor compounds of phosphodiesterase type 10a

The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Y 1 and Y 2 are adjacent atoms in Het 1 , which are independently selected from the group consisting of carbon and nitrogen; k is 0, 1, 2 or 3; Het 1 is a bivalent monocyclic 5- or 6-membered heteroaromatic radical, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N—R a as ring members, or a bivalent fused bicyclic 8-, 9- or 10-membered heteroaromatic radical, having 1, 2, 3 or 4 heteroatoms or heteroatom moieties selected from O, S, N and N—R a as ring members; Het 2 is inter alia monocyclic 5- or 6-membered hetaryl, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N—R 1a as ring members, Cyc is inter alia optionally substituted monocyclic 5- or 6-membered hetaryl or optionally substituted fused 8-, 9- or 10-membered bicyclic hetaryl; Ar is optionally substituted phenylene or optionally substituted bivalent 6-membered hetaryl; R is attached to a carbon atom of Het 1 and inter alia-halogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -alkoxy, C 1 -C 6 -fluoroalkyl, C 1 -C 6 -fluoroalkoxy, C 3 -C 6 -cycloalkyl etc.

SUBSTITUTED ISOXAZOLOPYRIDAZINONES AND ISOTHIAZOLOPYRIDAZINONES AND METHODS OF USE

Compounds of formula (I) 2. The compound or pharmaceutically acceptable salt or isotopically labelled form thereof of claim 1 , wherein{'sup': '1', 'sub': 1', '6', '2', '6', '2', '6', '3', '6, 'claim-text': [{'sub': 1', '6', '2', '6', '2', '6', '1', '6, 'C-Calkyl, C-Calkenyl, and C-Calkynyl are unsubstituted, partly or completely fluorinated and/or substituted with one or two substituents independently selected from the group consisting of C-Calkoxy, hydroxy, and oxo; and'}, {'sub': 3', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'C-Ccycloalkyl is unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of C-Calkyl, C-Calkoxy, fluorine, fluoroC-Calkyl, fluoroC-Calkoxy, hydroxy, and oxo.'}], 'Ris selected from the group consisting of C-Calkyl, C-Calkenyl, C-Calkynyl and C-Ccycloalkyl; wherein,'}3. The compound or pharmaceutically acceptable salt or isotopically labelled form thereof of claim 2 , wherein{'sup': '1', 'sub': 1', '6', '1', '6', '1', '4', '1', '4', '1', '3', '1', '3, 'Ris selected from the group consisting of C-Calkyl, fluoroC-Calkyl, C-C-alkoxy-C-C-alkyl and cyclopropyl, wherein cyclopropyl is unsubstituted or substituted with 1 or 2 substituents independently selected from the group consisting of C-Calkyl, fluorine, and fluoroC-Calkyl.'}4. The compound or pharmaceutically acceptable salt or isotopically labelled form thereof of ; wherein Ris phenyl; wherein phenyl is optionally substituted with 1 claim 1 , 2 claim 1 , 3 or 4 substituents selected from the group consisting of C-Calkyl claim 1 , C-Calkoxy claim 1 , fluoroC-Calkyl claim 1 , fluoroC-Calkoxy claim 1 , and halo.5. The compound or pharmaceutically acceptable salt or isotopically labelled form thereof of claim 1 , wherein Ris selected from the group consisting of methyl claim 1 , ethyl claim 1 , isopropyl claim 1 , n-propyl claim 1 , cyclopropyl claim 1 , methoxymethyl claim 1 , phenyl which is unsubstituted or substituted by halo.6. The ...

SUBSTITUTED PYRAZOLOPYRIMIDINES AND METHOD OF USE

Compounds of formula (I) 115.-. (canceled)18. The method according to claim 17 , wherein the condition or disorder is selected from the group consisting of pain claim 17 , substance abuse claim 17 , depression claim 17 , spasticity claim 17 , fragile X syndrome claim 17 , Down's syndrome claim 17 , autism claim 17 , retinal ganglion cell degeneration claim 17 , gastro-esophageal reflux disease (GERD) claim 17 , smoking cessation claim 17 , addiction of narcotic agents claim 17 , emesis claim 17 , cough claim 17 , overactive bladder claim 17 , anxiety claim 17 , migraine and tinnitus.19. The method according to claim 16 , wherein the substance abuse is alcohol dependence.20. The method according to claim 18 , wherein the substance abuse is alcohol dependence. This patent application is a divisional of U.S. patent application Ser. No. 15/133,851, filed Apr. 20, 2016, which claims priority to International Patent Application No. PCT/CN2015/076978 filed on Apr. 20, 2015, and European Patent Application No. 15168924.7 filed May 22, 2015. The entire contents of these applications are incorporated by reference into this patent application.The invention relates to substituted pyrazolopyrimidines that are positive allosteric modulators of the γ-aminobutyric acid receptor (e.g., GABA-B PAM), useful in treating diseases and conditions mediated and modulated by the γ-aminobutyric acid receptor B. Additionally, the invention relates to compositions containing compounds of the invention and processes of their preparation.The inhibitory neurotransmitter, γ-aminobutyric acid (GABA) exerts its actions through three distinct receptors—the ionotropic GABA-A and GABA-C receptors, and the metabotropic GABA-B receptor. The GABA-B receptor is a member of the class C family of GPCRs. The GABA-B receptor is an obligate heterodimer composed of a GABA-B1 and a GABA-B2 subunit (Bettler, B., et al. 2004; 84: 835-867). Notably, heterodimerization of the B1 and B2 subunits is required for proper ...

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 3. The compound of claim 1 , where Xis selected from O claim 1 , S claim 1 , —X═C(R)— claim 1 , where C(R) is bound to the carbon atom which carries R.4. The compound of claim 1 , where A is selected from A claim 1 , A claim 1 , Aand A.5. The compound of claim 1 , where Xis C—R.6. The compound of claim 5 , where Ris hydrogen or Y-Cyc.7. The compound of claim 1 , where Xis N.8. The compound of claim 1 , where Xis CH.9. The compound of claim 1 , where Xis S.10. The compound of claim 1 , where Xis O.11. The compound of claim 1 , where Xis C(R)═C(R).12. The compound of claim 1 , where Xis N═(CR).13. The compound of claim 11 , where Ris hydrogen or Y-Cyc.14. The compound of claim 1 , where Xis N═C(R).15. The compound of claim 11 , where Ris hydrogen.16. The compound of claim 1 , where Ris a radical Y-Cyc.17. The compound of claim 1 , where Ris selected from the group consisting of hydrogen claim 1 , fluorine claim 1 , C-C-alkyl claim 1 , C-C-fluoroalkyl claim 1 , C-C-alkoxy claim 1 , C-C-fluoroalkoxy claim 1 , cyclopropyl claim 1 , optionally substituted by 1 claim 1 , 2 or 3 methyl groups claim 1 , and fluorinated cyclopropyl.18. The compound of claim 17 , where Ris hydrogen.19. The compound of claim 1 , where A is A.20. The compound of claim 19 , where R claim 19 , Rare selected from hydrogen and fluorine.21. The compound of claim 19 , where Rand Rare claim 19 , independently of each other claim 19 , selected from the group consisting of hydrogen claim 19 , fluorine and methyl.22. The compound of claim 1 , where A is A.23. The compound of claim 1 , where A is ...

HETEROCYCLIC COMPOUNDS AND THEIR USE AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions. 2. A compound of general formula I according to claim 1 , corresponding enantiomeric claim 1 , diastereomeric and/or tautomeric forms thereof and/or the pharmaceutically acceptable salts thereof and/or the active ingredient precursors (prodrugs) thereof claim 1 , in which:{'sup': 1', '2, 'Rand Rindependently of one another denote'}hydrogen, a free electron pair, OH, CN or optionally substituted{'sub': 1', '6', '1', '6', '1', '6', '1', '6, 'O—C-Calkyl, C-Calkyl, CO—C-Calkyl, CO—OC-Calkyl.'}3. A one compound of general formula I according to claim 1 , corresponding enantiomeric claim 1 , diastereomeric and/or tautomeric forms thereof and/or the pharmaceutically acceptable salts thereof and/or the active ingredient precursors (prodrugs) thereof claim 1 , in which:{'sub': 1', '6', '3', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'claim-text': {'sub': 1', '6', '2', '1', '6', '1', '4', '3', '2', '1', '4', '1', '4', '1', '4', '2', '3', '2', '1', '4', '2', '1', '4', '2', '1', '4', '1', '4, '—N(C-Calkyl)-SO—C-Calkyl, C-Calkylene-CO—N(CH), C-Calkylene-CO—N-piperidyl, C-Calkylene-CO—N-morpholinyl, C-Calkylene-SO—N(CH), C-Calkylene-SO—N-piperidyl, C-Calkylene, SO—N-morpholinyl or C-Calkyl-O—C-Calkyl and'}, 'A denotes OH, —O—C-Calkyl, —OCF, —OCHFor optionally substituted —NH—C-Calkyl, —NH—CO—C-Calkyl, —NH—SO—C-Calkyl, —N(C-Calkyl), piperidinyl, morpholinyl, —N(C-Calkyl)-CO—C-Calkyl or'}{'sub': 3', '3', '2', '2', '1', '6', '2', '6', '2', '6', '3', ...

AIR SPRING ACTUATED SLIDER FOR SEMI-TRAILER

An air spring actuated slider pin release system for a semi-trailer slider includes an actuator shaft oriented to extend in generally parallel relationship to at least one of a pair of parallel main members, being connected to the slider for axial rotation, and having a transverse lever arm secured to each end of the shaft for common rotation. Each lever arm has an end connected to a retractable, biased lock pin via a link so that rotation of the shaft and the lever arms causes retraction of the associated lock pin relative to the main member. The actuator shaft has a normally projecting air spring bracket. An air spring is disposed between one of the main members and the air spring bracket so that inflation of the air spring acts on the air spring bracket, axially rotating the shaft and the lever arms for retracting the lock pins. 1. An air spring actuated slider pin release system for a semi-trailer slider having a pair of main members extending along a longitudinal axis of the slider , and at least one cross member separating the main members in spaced , parallel relationship to each other , comprising:an actuator shaft oriented to extend in a generally parallel relationship to at least one of the main members, being connected to said slider for axial rotation, and having a transverse lever arm secured to each end of said shaft for common rotation;each said lever arm having an end connected to a retractable, biased lock pin so that rotation of said shaft and said lever arms causes retraction of said associated lock pin relative to the main member;said actuator shaft having a normally projecting air spring bracket; andan air spring disposed in operational relationship to said air spring bracket so that inflation of said air spring directly acts on said air spring bracket, [moving said bracket transversely to said main members and] axially rotating said shaft and said lever arms for retracting said lock pins.2. The slider pin release system of claim 1 , wherein ...

PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY

The present invention relates to phenalkylamine derivatives of the formula (I)

Novel inhibitor compounds of phosphodiesterase type 10A

The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: 2. The compound of claim 1 , where{'sup': 1', '3', 'y', 'y', 'y', 'y', 'y', 'y, 'sub': 2', '2', '2', '2', '2', '2', '2', '1', '4', '1', '4', '1', '4', '1', '4, 'Y, Yindependently of each other are selected from the group consisting of a chemical bond, CH, O, O—CH, C(O)O, C(O), NR, NR—CH, S(O)—NR, C(O)—NR, S, S(O), S(O), C(O)—O—CH, C(O)—NR—CH, 1,2-ethanediyl, 1,2-ethenediyl and 1,2-ethynediyl, where Ris selected from the group consisting of hydrogen, C-C-alkyl, C-C-alkylcarbonyl, C-C-alkylsulfonyl, and C-C-fluoroalkylsulfonyl.'}3. The compound of claim 1 , where Xis S.4. The compound of claim 1 , where Xis N.5. The compound of claim 1 , where Xis CH.6. The compound of claim 1 , where Yis selected from the group consisting of a chemical bond claim 1 , O claim 1 , NH claim 1 , CH claim 1 , 1 claim 1 ,2-ethenyl claim 1 , ethynyl claim 1 , C(O) claim 1 , NHCH claim 1 , C(O)NH and C(O)NHCH.7. The compound of claim 1 , where Cycis selected from the group consisting of saturated 4- claim 1 , 5- claim 1 , 6- claim 1 , 7- or 8-membered heteromonocycles and saturated 7- claim 1 , 8- claim 1 , 9- or 10-membered heterobicycles claim 1 , where the heteromonocycles and the heterobicycles have one nitrogen or oxygen atom as ring member and may have one further heteroatom or heteroatom group as ring member claim 1 , which is selected from the group consisting of O claim 1 , S claim 1 , S(═O) claim 1 , S(═O)and N claim 1 , where the saturated heteromonocycle and the saturated heterobicycle are unsubstituted or carry 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 radicals Ror one radical Y′—Rand 0 claim 1 , 1 claim 1 , 2 claim 1 , 3 or 4 radicals R claim 1 , where R claim 1 , Rand Y′ are as defined in .8. The compound of claim 7 , where Ris selected from the group consisting of 1-piperidinyl claim 7 , 4 claim 7 ,4-difluoro-1-piperidinyl ...

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: 2. The compound of claim 1 , where A is C(R claim 1 ,R).3. The compound of claim 2 , where A is CH.4. The compound of any of claim 1 , where X is C(O).5. The compound of claim 4 , where Y is C(R claim 4 ,R).6. The compound of claim 4 , where Rand R claim 4 , independently of each other claim 4 , are selected from the group consisting of hydrogen claim 4 , fluorine and methyl.7. The compound of claim 1 , where Y is C(O).81. The compound of claim 1 , where Z is a bond.10. The compound of claim 1 , where Ris selected from the group consisting of saturated 4- claim 1 , 5- claim 1 , 6- claim 1 , 7- or 8-membered heteromonocycles and saturated 7- claim 1 , 8- claim 1 , 9- or 10-membered heterobicycles claim 1 , where the heteromonocycles and the heterobicycles have one nitrogen or oxygen atom as ring member and may have one further heteroatom or heteroatom containing group as ring member claim 1 , which is selected from the group consisting of O claim 1 , S claim 1 , S(═O) claim 1 , S(═O)and N claim 1 , where the saturated heteromonocycle and the saturated heterobicycle are unsubstituted or carry 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 radicals Ror one radical Y′—Rand 0 claim 1 , 1 claim 1 , 2 claim 1 , 3 or 4 radicals R claim 1 , where R claim 1 , Rand Y′ are as defined in .11. The compound of claim 10 , where Z—Ris independently selected from the group consisting of 1-piperidinyl claim 10 , 4 claim 10 ,4-difluoro-1-piperidinyl claim 10 , 4-hydroxylpiperidin-1-yl claim 10 , 4-piperidinyl claim 10 , 1-methyl-4-piperidinyl claim 10 , 1-piperazinyl claim 10 , 4-methyl-1-piperazinyl claim 10 , 4-(tert.-butyloxycarbonyl)piperazin-1-yl claim 10 , 1-piperazinylmethyl claim 10 , 4-methyl-1-piperazinylmethyl claim 10 , 1-piperazinylcarbonyl claim 10 , 4-methyl-1-piperazinylcarbonyl claim 10 , morpholin-4-yl claim 10 , morpholin-4 ...

SUBSTITUTED PYRAZOLOPYRIMIDINES AND METHOD OF USE

Compounds of formula (I) 2. The compound or pharmaceutically acceptable salt of wherein:{'sup': 1', '5', '6', '5', '6, 'sub': m', '1', '6, 'Lis —(CRR)—, wherein m is 1 and wherein Rand Rare, at each occurrence, independently selected from the group consisting of hydrogen and C-Calkyl.'}3. The compound or pharmaceutically acceptable salt of wherein Ris hydrogen and Ris C-Calkyl.4. The compound or pharmaceutically acceptable salt of claim 1 , wherein{'sup': 1', 'G, 'Gis selected from the group consisting of 5-6-membered heteroaryl and phenyl; wherein the 5-6-membered heteroaryl and phenyl are unsubstituted or carry 1, 2, 3 or 4 radicals R.'}5. The compound or pharmaceutically acceptable salt of claim 1 , wherein{'sup': '1', 'Gis selected from the group consisting of phenyl, 3-chlorophenyl, 4-chlorophenyl, 4-(trifluoromethyl)phenyl, pyridine-2-yl and 5-chloropyridin-2-yl.'}6. The compound or pharmaceutically acceptable salt of claim 1 , wherein:{'sup': '3', 'Ris hydrogen; and'}{'sup': '4', 'sub': 1', '6, 'Ris C-Calkyl.'}7. The compound or pharmaceutically acceptable salt of claim 1 , wherein:{'sup': '1', 'sub': 1', '6', '2', '6', '2', '6', '3', '6', '3', '6', '1', '6', '1', '6, 'claim-text': [{'sub': 1', '6', '2', '6', '2', '6', '1', '6', '3', '6', '1', '6', '1', '6', '1', '6, 'sup': '1a', 'a) the C-Calkyl, the C-Calkenyl, the C-Calkynyl, the C-Calkyl of C-CcycloalkylC-Calkyl, and the C-Calkyl of 4-7-membered heterocycleC-Calkyl are unsubstituted or substituted with one or more substituents R;'}, {'sub': 3', '6', '3', '6', '3', '6', '1', '6', '1', '6, 'sup': '1b', 'b) the C-Ccycloalkyl, the C-Ccycloalkyl of C-CcycloalkylC-Calkyl, 4-7-membered heterocycle, and the 4-7-membered heterocycle of 4-7-membered heterocycleC-Calkyl are unsubstituted or substituted with one or more substituents R; and'}], 'Ris selected from the group consisting of C-Calkyl, C-Calkenyl, C-Calkynyl, C-Ccycloalkyl, C-CcycloalkylC-Calkyl, 4-7-membered heterocycle and 4-7-membered heterocycleC-Calkyl ...

WRAP AROUND AXLE CONNECTION FOR SUSPENSION TRAILING ARM

A vehicle suspension is provided, including an axle having an axle body with an exterior surface, a main trailing arm shell portion having a first axle engagement surface configured for engaging a first portion of the exterior surface, and a second trailing arm shell portion having a second axle engagement surface configured for engaging a second portion of the exterior surface. Upon assembly to the axle, the main trailing arm shell portion and the second trailing arm shell portion engage more than 180° of a curvature of the exterior surface. 1. A vehicle suspension , comprising:an axle having an axle body with an exterior surface;a main trailing arm shell portion having a first axle engagement surface configured for engaging a first portion of said exterior surface;a second trailing arm shell portion having a second axle engagement surface configured for engaging a second portion of said exterior surface;upon assembly to said axle, said main trailing arm shell portion and said second trailing arm shell portion engaging more than 180° of a curvature of said exterior surface.2. The suspension of claim 1 , wherein said axle exterior surface is circular when viewed in cross-section claim 1 , and each said first and second axle engagement surfaces are arcuate in shape to complement said exterior surface.3. The suspension of claim 1 , wherein said first axle engagement surface extends over a greater portion of said axle exterior surface than said second axle engagement surface.4. The suspension of claim 1 , wherein said main trailing arm shell portion is longer in a direction transverse to said axle than said second trailing arm shell portion.5. The suspension of claim 1 , wherein said main and said second trailing arm shell portions have complementary mating alignment formations.6. The suspension of claim 6 , wherein said complementary mating alignment formations include a mating tab and slot on opposing surfaces of said main and second shell portions.7. The suspension ...

AIR SPRING ACTUATED SLIDER FOR SEMI-TRAILER

An air spring actuated slider pin release system for a semi-trailer slider includes an actuator shaft oriented to extend in generally parallel relationship to at least one of a pair of parallel main members, being connected to the slider for axial rotation, and having a transverse lever arm secured to each end of the shaft for common rotation. Each lever arm has an end connected to a retractable, biased lock pin via a link so that rotation of the shaft and the lever arms causes retraction of the associated lock pin relative to the main member. The actuator shaft has a normally projecting air spring bracket. An air spring is disposed between one of the main members and the air spring bracket so that inflation of the air spring acts on the air spring bracket, axially rotating the shaft and the lever arms for retracting the lock pins. 1. An air spring actuated slider pin release system for a semi-trailer slider having a pair of main members extending along a longitudinal axis of the slider , and at least one cross member separating the main members in spaced , parallel relationship to each other , comprising:an actuator shaft oriented to extend in generally parallel relationship to at least one of the main members, being connected to said slider for axial rotation, and having a transverse lever arm secured to each end of said shaft for common rotation;each said lever arm having an end connected to a retractable, biased lock pin so that rotation of said shaft and said lever arms causes retraction of said associated lock pin relative to the main member;said actuator shaft having a normally projecting air spring bracket; andan air spring disposed between one of the main members and said air spring bracket so that inflation of said air spring acts on said air spring bracket, axially rotating said shaft and said lever arms for retracting said lock pins.2. The slider pin release system of claim 1 , wherein said air spring acts directly on said actuator shaft via said air ...

SUBSTITUTED ISOXAZOLOPYRIDAZINONES AND ISOTHIAZOLOPYRIDAZINONES AND METHODS OF USE

Compounds of formula (I) 126.-. (canceled)28. The compound or pharmaceutically acceptable salt of claim 27 , wherein{'sup': '1', 'sub': 1', '6', '2', '6', '2', '6', '3', '6, 'claim-text': [{'sub': 1', '6', '2', '6', '2', '6', '1', '6, 'C-Calkyl, C-Calkenyl, and C-Calkynyl are unsubstituted, partly or completely fluorinated and/or substituted with one or two substituents independently selected from the group consisting of C-Calkoxy, hydroxy, and oxo; and'}, {'sub': 3', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'C-Ccycloalkyl is unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of C-Calkyl, C-Calkoxy, fluorine, fluoroC-Calkyl, fluoroC-Calkoxy, hydroxy, and oxo.'}], 'Ris selected from the group consisting of C-Calkyl, C-Calkenyl, C-Calkynyl and C-Ccycloalkyl; wherein,'}29. The compound or pharmaceutically acceptable salt of claim 27 , wherein Ris phenyl optionally substituted with 1 claim 27 , 2 claim 27 , 3 or 4 substituents selected from the group consisting of C-Calkyl claim 27 , C-Calkoxy claim 27 , fluoroC-Calkyl claim 27 , fluoroC-Calkoxy claim 27 , and halo.30. The compound or pharmaceutically acceptable salt of claim 27 , wherein Ris selected from the group consisting of methyl; ethyl; isopropyl; n-propyl; cyclopropyl; methoxymethyl; and phenyl claim 27 , which is unsubstituted or substituted by halo.31. The compound or pharmaceutically acceptable salt of claim 27 , wherein{'sup': '3', 'sub': 1', '6', '3', '6, 'claim-text': [{'sub': 1', '6, 'C-Calkyl is unsubstituted, partly or completely fluorinated and/or substituted with one or two substituents independently selected from the group consisting of C1-C6alkoxy, hydroxy, and oxo; and'}, {'sub': 3', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'C-Ccycloalkyl is unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of C-Calkyl, C-Calkoxy, fluorine, fluoroC-Calkyl, fluoroC-Calkoxy, hydroxy, and ...

Extracorporeal blood treatment machine comprising a poka-yoke for a pressure sensor

The present invention relates to an extracorporeal blood treatment machine, i.e. a dialysis machine (1), comprising a blood treatment device (2), a conveying device (4) for conveying blood through the blood treatment device (2), and a connection mask (6) which is designed to interchangeably receive an adapted tube set (8) in a predefined arrangement on the blood treatment machine (1). The tube set (8) has pressure-monitoring lines (14, 16, 18) which each branch off from said tube set at a branch (20, 22, 24) and can be connected to pressure sensor connections (26, 28, 30) located on the connection mask (6) of the blood treatment machine. The pressure sensor connections (26, 28, 30) are spaced apart from one another and positioned on the extracorporeal blood treatment machine (1) so as to match the tube set (8) such that, when the tube set (8) is mounted in the predefined arrangement on the connection mask (6), each pressure-monitoring line (14, 16, 18), owing to its limited length and the predefined arrangement of the associated branch (20, 22, 24) on the blood treatment machine (1), can be connected exclusively to in each case one of the pressure sensor connections (26, 28, 30). The invention also relates to a corresponding tube set (8) for use with a dialysis machine (1).

NEW COMPOUNDS INHIBITING TYPE 10A PHOSPHODIESTERASE

SE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (I) DONDE X1 ES N O CR1; X2 ES N O CR2; X3 ES N O CR3; X4 ES N O CR4, EN DONDE R1 Y R4 SON CADA UNO H, HALOGENO, ALQUILO(C1-C4), ENTRE OTROS; R2 Y R3 SON CADA UNO H, OH, ALCOXI(C1-C4)-ALQUILO(C1-C4), ENTRE OTROS; A ES O, S, S(=O), S(=O)2, ENTRE OTROS; Het ES FENILO, HETARILO MONOCICLICO O HETARILO BICICLICO; R7, R8, R9 Y R10 SON CADA UNO H, HALOGENO, ALQUILO(C1-C4), FLUOROALCOXI(C1-C4), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 4-PIRIDIN-4-IL-2-(2-QUINOLIN-2-IL-ETIL)-1,2-DIHIDRO-PIRROLO[3,4-c]PIRIDIN-3-ONA; 7-PIRIDIN-4-IL-2-(2-QUINOLIN-2-IL-ETIL)-2,3-DIHIDRO-PIRROLO[3,4-c]PIRIDIN-1-ONA; 3,3-DIFLUORO-7-PIRIDIN-4-IL-2-(2-QUINOLIN-2-IL-ETIL)-2,3-DIHIDRO-ISOINDOL-1-ONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA FOSFODIESTERASA TIPO 10A SIENDO UTILES EN EL TRATAMIENTO DE ESQUIZOFRENIA, TRASTORNO BIPOLAR, DEPRESION, ENFERMEDAD DE ALZHEIMER

Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy

Novel inhibitor compounds of phosphodiesterase type 10a

The present invention relates to compounds of the formula (I), the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

Inhibitors of phosphodiesterase type 10a

The present invention relates to novel compounds of the formula (I) which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Q is O or S, X1 is N or CH, X2 is N or C-R7; X3 is O, S, -X4=C(R8)-, where C(R8) is bound to the carbon atom which carries R2, or -X5=C(R9)-, where X5 is bound to the carbon atom which carries R2; X4 is N or C-R9; X5 is N; Het is selected from optionally substituted phenyl, monocyclic hetaryl and fused bicyclic hetaryl; R1 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkylsulfanyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4- alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, the moiety Y1-Cyc1; R2 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4- alkoxy-C1-C4-alkoxy, C2-C4-alkenyloxy, etc; A represents one of the following groups A1, A2, A3, A4 or A5: where * indicates the points of attachment to Het and to the nitrogen atom, respectively; and where R3 to R9, R3e, R3f, A', Y1 and Cyc1 are defined in the claims.

Tetraline and indane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.

Novel inhibitor compounds of phosphodiesterase type 10A

The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

heterocyclic compounds, pharmaceutical compositions containing them, and their uses as glycine transporter inhibitors 1

Novel inhibitor compounds of phosphodiesterase type 10A

本發明係關於新穎羧醯胺化合物、含有該等羧醯胺化合物之醫藥組合物及其在療法中之用途。該等化合物具有有價值的治療特性，且尤其適於治療或控制選自神經病症及精神病症之醫學病症，適於改善與該等病症有關之症狀，及適於降低該等病症之風險。

new phosphoestearase inhibitor compounds type 10a

resumo novos compostos inibidores da fosfoestearase tipo 10a a presente invenção refere-se a compostos da fórmula (i), os seus n-óxidos, tautômeros, as prodrogas e os seus sais farmaceuticamente aceitáveis. na fórmula i, as variáveis het, a, x, y, z, r1, r2, r3, r4, r5 e q são como definido nas reivindicações. os compostos da fórmula i, os seus n-óxidos, tautômeros, as prodrogas e os seus sais farmaceuticamente aceitáveis são inibidores da fosfodiesterase tipo 10a. assim, a invenção também está relacionada com a utilização dos compostos da fórmula i, seus n-óxidos, tautômeros, prodrogas e os seus sais farmaceuticamente aceitáveis para o fabrico de um medicamento e que, os quais são, portanto, adequados para o tratamento ou controle de desordens médicas selecionadas a partir de perturbações neurológicas e perturbações psiquiátricas, para melhorar os sintomas associados com tais perturbações e para reduzir o risco de tais desordens.

INHIBITING COMPOUNDS OF TYPE 10A PHOSPHODESTERASE

Estos compuestos, los N-óxidos, los tautómeros, las prodrogas y las sales farmacéuticamente aceptables de los mismos son inhibidores de la fosfodiesterasa de tipo 10A y su uso en la elaboración de un medicamento los vuelve adecuados para tratar o controlar los trastornos médicos seleccionados entre trastornos neurológicos y trastornos psiquiátricos, para aliviar los síntomas asociados con dichos trastornos y para reducir el riesgo de dicho trastornos. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque, en la fórmula (1), las variables X, Y, Q¹, Q², R¹ y R² tienen los siguientes significados: X es C-R³ o N; Q¹ es S u O y Q² es C-R⁴ o N y Q² está conectado a X a través de una unión doble mientras que Q¹ está conectado a X a través de una unión simple; o Q² es S u O y Q¹ es C-R⁴ o N y Q¹ está conectado a X a través de una unión doble mientras que Q² está conectado a X a través de una unión simple; Y es C-R⁵ o N; R¹ se selecciona entre el grupo que consiste en: hidrógeno, halógeno, ciano, nitro, R¹¹, OH, OR¹², S(O)qR¹³, C(O)H, C(O)R¹⁴, C(O)OH, C(O)OR¹⁵, OC(O)R¹⁶, Y¹-NR¹⁷R¹⁸, Y¹-N(R¹⁹)-Y³-NR¹⁷R¹⁸, Y¹-N(R¹⁹)-Y²-R¹⁵ᵃ y una unidad Z¹-Ar¹; R² se selecciona entre el grupo que consiste en: hidrógeno, halógeno, ciano, nitro, R²¹, OH, OR²², S(O)qR²³, C(O)H, C(O)R²⁴, C(O)OH, C(O)OR²⁵, OC(O)R²⁶, Y¹-NR²⁷R²⁸, Y¹-N(R²⁹)-Y³-NR²⁷R²⁸, Y¹-N(R¹⁹)-Y²-R²⁵ᵃ y una unidad Z²-Ar²; con la condición de que por lo menos uno de R¹ y R² debe ser diferente de hidrogeno; R³ se selecciona entre el grupo que consiste en: hidrógeno, halógeno, ciano, nitro, R³¹, OR³², S(O)qR³³, C(O)H, C(O)R³⁴, C(O)OH, C(O)OR³⁵, OC(O)R³⁶, Y¹-NR³⁷R³⁸, Y¹-N(R³⁹)-Y³-NR³⁷R³⁸, Y¹-N(R³⁹)-Y²-R³⁵ᵃ y una unidad Z³-Ar³; R⁴ se selecciona entre el grupo que consiste en: hidrógeno, halógeno, ciano, nitro, R⁴¹, OR⁴², S(O)qR⁴³, C(O)H, C(O)R⁴⁴, C(O)OH, C(O)OR⁴⁵, OC(O)R⁴⁶, Y¹-NR⁴⁷R⁴⁸, Y¹-N(R⁴⁹)-Y³-NR⁴⁷R⁴⁸, Y¹-N(R⁴⁹)-Y²-R⁴⁵ᵃ y una unidad Z⁴-Ar⁴; R⁵ se selecciona entre el grupo que consiste en: hidrógeno, halógeno, ciano, ...

Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GIyT1 inhibitors.

Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.

Guanidine compounds and use of same as binding partners for 5-HT5 receptors

Guanidine compounds (I), their enantiomers, diastereomers and/or tautomers and salts are new. Guanidine compounds of formula (I), their enantiomers, diastereomers and/or tautomers and salts are new. Q-N(R 2>)-C(=NR 3>)-N(R 1>)-Z-W (I) W : substituted phenyl or thienyl; Z : -(CR 1> zR 2> z) a-(V z) b-(CR 3> zR 4> z) c-; a and c : 0-4; b : 0 or 1, and the sum of a, b and c = 1-5; R 1> z to R 4> z : hydrogen, halo, hydroxy, 1-6C alkyl, 2-6C alkenyl or alkynyl, 1-6C alkylene(3-7C)cycloalkyl, 3-7C cycloalkyl, (hetero)aryl, 1-4C alkylene(hetero)aryl or R 1> z/R 2> z and/or R 3> z/R 4> z together complete a 3-7 membered, optionally substituted, (un)saturated carbo- or heterocyclic group, containing up to 3 heteroatoms (O, N or S); V z : CO, CONR 5> z, NR 5> zCO, O, S, SO, SO 2, SO 2NR 5> z, NR 5> zSO 2, CS, CSNR 5> z, NR 5> zCS, CSO, OCS, COO, OCO, O, ethylnylene, C(=CR 6> zR 7> z), CR 6> z=CR 7> z, NR 5> zCONR 5>, OCONR 5> z or NR 5> z; R 1>-R 3> : hydrogen or substituents; Q : disubstituted 5-membered heteroaryl. Full definitions are given in the DEFINITIONS (Full Definitions) field. ACTIVITY : Antimigraine; Neuroprotective; Nootropic; Cerebroprotective; Anticonvulsant; Neuroleptic; Tranquilizer; Antidepressant; Cytostatic; Analgesic; Antialcoholic. No details of tests for these activities are given. MECHANISM OF ACTION : 5-Hydroxytryptamine (5HT) class 5 receptor non-competitive inhibitor. (I) bind to 5-hydroxytryptamine (5HT) class 5 receptors as non-competitive inhibitors, so cause (ultimately) an increase in intracellular calcium ion concentration. The compound N-(2-methoxybenzyl)-N'-(1,3-thiazol-2-yl)guanidine (Ia) had binding affinity (inhibition constant) for human 5-HT 5 receptors of below 50 nM.

Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GIyT1 inhibitors.

Inhibitors of phosphodiesterase type 10a 10a

Novel inhibitor compounds of phosphodiesterase type 10a

The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. where in formula I the variables X, Y, Q1, Q2 have the following meanings: X is C-R3 or N; Q1 is S or O and Q2 is C-R4 or N and Q2 is connected to X via a double bond while Q1 is connected to X via a single bond; or Q2 is S or O and Q1 is C-R4 or N and Q1 is connected to X via a double bond while Q2 is connected to X via a single bond; Y is C-R5 or N; where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

Air spring actuated slider for semi-trailer

An air spring actuated slider pin release system for a semi-trailer slider includes an actuator shaft oriented to extend in generally parallel relationship to at least one of a pair of parallel main members, being connected to the slider for axial rotation, and having a transverse lever arm secured to each end of the shaft for common rotation. Each lever arm has an end connected to a retractable, biased lock pin via a link so that rotation of the shaft and the lever arms causes retraction of the associated lock pin relative to the main member. The actuator shaft has a normally projecting air spring bracket. An air spring is disposed between one of the main members and the air spring bracket so that inflation of the air spring acts on the air spring bracket, axially rotating the shaft and the lever arms for retracting the lock pins.

Novel inhibitor compounds of phosphodiestarase type 10a

Method for producing prepolymers containing isocyanate groups and urethane groups

Novel inhibitor compounds of phosphodiesterase type 10a

Substituted pyrazolopyrimidines and method of use

Compounds of formula (I) (I) and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , L 1 and G 1 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the γ-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.

Heterocyclic carboxamides useful as inhibitors of phosphodiesterase type 10a.

Nuevos compuestos inhibidores de fosfodiesterasa del tipo 10A. La presente invención se relaciona con compuestos que son inhibidores de fosfodiesterasa del tipo 10A y con su uso en la fabricación de un medicamento y los cuales de esta manera son apropiados para tratar o controlar trastornos médicos que se seleccionan entre trastornos neurológicos y trastornos psiquiátricos, para mejorar los síntomas asociados con dichos trastornos y para reducir el riesgo de dichos trastornos. (ver Fórmula).

Air spring actuated slider for semi-trailer

An air spring actuated slider pin release system for a semi-trailer slider includes an actuator shaft oriented to extend in generally parallel relationship to at least one of a pair of parallel main members, being connected to the slider for axial rotation, and having a transverse lever arm secured to each end of the shaft for common rotation. Each lever arm has an end connected to a retractable, biased lock pin via a link so that rotation of the shaft and the lever arms causes retraction of the associated lock pin relative to the main member. The actuator shaft has a normally projecting air spring bracket. An air spring is disposed between one of the main members and the air spring bracket so that inflation of the air spring acts on the air spring bracket, axially rotating the shaft and the lever arms for retracting the lock pins.

Isoindoline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to isoindoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such isoindoline derivatives, and the use of such isoindoline derivatives for therapeutic purposes.

Tetrahydroisoquinolines, pharmaceutical compositions containing them, and their use in therapy

Tetrahidroisoquinolina de la fórmula (I) en donde R es R1-W-A1-Q-Y-A2-X-; R1 es hidrógeno, C1-C6-alquilo, C1-C6-alquilo halogenado, hidroxi-C1-C4-alquilo, C1-C6-alcoxi-C1-C4-alquilo, amino-C1-C4-alquilo, C1-C6-alquilamino-C1-C4-alquilo, di-C1-C6-alquilamino-C1-C4-alquilo, C1-C6-alquilcarbonilamino-C1-C4-alquilo, C1-C6-alquiloxicarbonilamino-C1-C4-alquilo, C1-C6-alquilaminocarbonilamino-C1-C4-alquilo, di-C1-C6-alquilaminocarbonilamino-C1-C4alquilo, C1-C6-alquilsulfonilamino-C1-C4-alquilo, (C6-C12-aril-C1-C6-alquil)amino-C1-C4-alquilo, C6-C12-aril-C1-C4-alquilo opcionalmente sustituido, C3-C12-heterociclil-C1-C4-alquilo opcionalmente sustituido, C3-C12-cicloalquilo, C1-C6-alquilcarbonilo, halogenado C1-C6-alquilcarbonilo, C1-C6-alcoxicarbonilo, halogenado C1-C6-alcoxicarbonilo, C6-C12-ariloxicarbonilo, aminocarbonilo, C1-C6-alquilaminocarbonilo, (C1-C4-alquil halogenado)aminocarbonilo, C6-C12-arilaminocarbonilo, C2-C6-alquenilo, C2-C6-alquinilo, C6-C12-arilo opcionalmente sustituido , hidroxi, C1-C6-alcoxi, halogenado C1-C6-alcoxi, C1-C6-alquilcarboniloxi, C1-C6-hidroxialcoxi, C1-C6-alcoxi-C1-C4-alcoxi, amino-C1-C4-alcoxi, C1-C6-alquilamino-C1-C4-alcoxi, di-C1-C6-alquilamino-C1-C4-alcoxi, C1-C6-alquilcarbonilamino-C1-C4-alcoxi, C6-C12-arilcarbonilamino-C1-C4-alcoxi, C1-C6-alcoxicarbonilamino-C1-C4-alcoxi, C6-C12-aril-C1-C4-alcoxi, C1-C6-alquilsulfonilamino-C1-C4-alcoxi, (C1-C6-alquil halogenado)sulfonilamino-C1-C4-alcoxi, C6-C12-sulfonilamino-C1-C4-alcoxi, (C6-C12-aril-C1-C6-alquil)sulfonilamino-C1-C4-alcoxi, C3-C12-heteroarilalquilo opcionalmente sustituido, sulfonilamino-C1-C4-alcoxi opcionalmente sustituido, C3-C12-heteroarilalquilo 20 opcionalmente sustituido-C1-C4-alcoxi, C6-C12-ariloxi, C3-C12-heteroarilalquilooxi opcionalmente sustituido, C1-C6-alquiltio, C1-C6-alquiltio halogenado, C1-C6-alquilamino, (C1-C6-alquil halogenado)amino, di-C1-C6-alquilamino, di-( C1-C6-alquil halogenado)amino, C1-C6-alquilcarbonilamino, (C1-C6-alquil halogenado)carbonilamino, C6- ...

INHIBITING COMPOUNDS OF TYPE 10A PHOSPHODESTERASE

Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) donde Q es O ó S; X¹ es N o CH; X² es N o C-R⁷; X³ es O, S, -X⁴=C(R⁸)-, donde C(R⁸) está unido al átomo de carbono que se une a R² o -X⁵=C(R⁹)-, donde X⁵ está unido al átomo de carbono que se une a R²; X⁴ es N o C-R⁹; X⁵ es N; Het se selecciona entre i) hetarilo monocíclico con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, que no está sustituido o puede tener 1, 2, 3 ó 4 sustituyentes idénticos o diferentes Rˣ, ii) hetarilo bicíclico fusionado con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, benzotienilo o benzofurilo, donde hetarilo bicíclico, benzotienilo y benzofurilo, en forma independiente entre sí, no están sustituidos o pueden tener 1, 2, 3 ó 4 sustituyentes idénticos o diferentes Rˣ, y iii) fenilo, que se une a un radical hetarilo monocíclico con 1 ó 2 átomos de nitrógeno y opcionalmente un heteroátomo adicional seleccionado entre O, S y N como miembros del anillo, que además de hetarilo monocíclico, puede tener 1, 2 ó 3 sustituyentes idénticos o diferentes Rˣ, donde Rˣ se selecciona entre el grupo que consiste en H, halógeno, alquilo C₁₋₄, alcoxi C₁₋₄, fluoroalquilo C₁₋₄, fluoroalcoxi C₁₋₄, cicloalquilo C₃₋₆, alcoxi C₁₋₄-alcoxi C₁₋₄, alcoxi C₁₋₄-alquilo C₁₋₄, OH, hidroxi-alquilo C₁₋₄, O-cicloalquilo C₃₋₆, benciloxi, C(O)O-(alquilo C₁₋₄), O-(alquil C₁₋₄)-CO₂H, N(Rˣ¹)(Rˣ²), C(O)N(Rˣ¹)(Rˣ²), alquil C₁₋₄-N(Rˣ¹)(Rˣ²), -NRˣ³-C(O)-N(Rˣ¹)(Rˣ²), NRˣ³-C(O)O-(alquilo C₁₋₄), -N(Rˣ³)-SO₂-Rˣ⁴, fenilo, CN, -SF₅, -OSF₅, -SO₂Rˣ⁴, -SRˣ⁴ y trimetilsililo, donde Rˣ¹, Rˣ², Rˣ³ y Rˣ⁴, en forma independiente entre sí se seleccionan entre el grupo que consiste en hidrógeno, alquilo C₁₋₄, fluoroalquilo C₁₋₄ y cicloalquilo C₃₋₆ o Rˣ¹ y Rˣ² forman junto con el átomo de N al cual están unidos un heterociclo con nitrógeno de entre 3 y 7 miembros que puede tener 1, 2 ó ...

5-ring heteroaromatic compounds and their use as binding partners for 5-ht5 receptors

The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for treating and/or preventing diseases, and to medicaments containing them.

Fused heterocyclic compounds as s1p modulators

The invention relates to heterocyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.

Guanidine compounds, and use thereof as binding partners for 5-ht5 receptors

The invention relates to guanidine compounds of general formula (I), corresponding enantiomeric, diastereomeric, and/or tautomeric forms thereof, and pharmaceutically acceptable salts thereof. The invention further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors in order to treat diseases modulated by 5-HT5 receptor activity, especially treat neurodegenerative and neuropsychiatric disorders and the signs, symptoms, and malfunctions associated therewith.

Fused heterocyclic compounds as S1P modulators

The invention relates to heterocyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.

Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy.

La presente invención se refiere a derivados de aminotetralina de fórmula (I) o una sal fisiológicamente aceptable de lo mismo. La invención se refiere a composiciones farmacéuticas que comprenden tales derivados de aminotetralina, y el uso de tales derivados de aminotetralina con propósitos terapéuticos. Los derivados de aminotetralina son inhibidores de GlyT1.

Wrap around axle connection for suspension trailing arm

A vehicle suspension is provided, including an axle having an axle body with an exterior surface, a main trailing arm shell portion having a first axle engagement surface configured for engaging a first portion of the exterior surface, and a second trailing arm shell portion having a second axle engagement surface configured for engaging a second portion of the exterior surface. Upon assembly to the axle, the main trailing arm shell portion and the second trailing arm shell portion engage more than 1800 of a curvature of the exterior surface.

Aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminoindane derivatives of the Formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane deriva- tives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.

Guanidine compounds, and use thereof as binding partners for 5-ht5 receptors

The invention relates to guanidine compounds of general formula (I), corresponding enantiomeric, diastereomeric, and/or tautomeric forms thereof, and pharmaceutically acceptable salts thereof. The invention further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors in order to treat diseases modulated by 5-HT5 receptor activity, especially treat neurodegenerative and neuropsychiatric disorders and the signs, symptoms, and malfunctions associated therewith.

Heterocyclic compounds, pharmaceutical compositions containing them, and their use as inhibitors of the glycine transporter 1

The present invention relates to heterocyclic compounds of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such heterocyclic compounds, and the use of such heterocyclic compounds for the manufacture of a medicament for inhibiting the glycine transporter GIyT1.

4-benzylaminoquinolines, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to 4-benzylaminoquinolines of the formula (I) or physiologically tolerated salts thereof. The invention relates to pharmaceutical compositions comprising such quinolines, and the use of such quinolines for therapeutic purposes. The quinolines are GIyTI inhibitors.

Tetrahydroisoquinolines, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GIyT1 inhibitors.

Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy

608314 Disclosed is a cyano substituted aminotetraline derivative of formula (I) where the substituents are as disclosed in the specification. Examples of compounds of formula (I) are: 7-Amino-8-(3,4-dichlorobenzyl)-5,6,7,8-tetrahydronaphthalene-2-carbonitrile; 7-Amino-8-(4-chlorobenzyl)-5,6,7,8-tetrahydronaphthalene-2-carbonitrile; Ethyl [7-cyano-1-(3,4-dichlorobenzyl)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamate and tert-Butyl [7-cyano-1-(3,4-dichlorobenzyl)-1,2,3,4-tetrahydronaphthalen-2-yl]carbamate. Also disclosed are pharmaceutical compositions comprising a compound of formula (I) and the use of a compound of formula (I) in the manufacture of a medicament for inhibiting glycine transporter GlyT1 useful in treating neurologic or psychiatric disorder or pain such as dementia, cognitive impairment, or attention deficit disorder, anxiety disorder, a mood disorder such as depression, a bipolar disorder, schizophrenia, or a psychotic disorder.

AMINOTETRALINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM, AND THEIR USES IN THERAPY

Derivados de aminotetralina de la fórmula (I), o una sal fisiológicamente tolerable de los mismos. La invención se relaciona con composiciones farmacéuticas que comprenden dichos derivados de aminotetralina, y el uso de dichos derivados de aminotetralina con propósitos terapéuticos. Los derivados de aminotetralina son inhibidores de GlyT1.

Hetaryl-substituted guanidine compounds and use thereof as binding partners for 5-ht5-receptors

Die vorliegende Erfindung betrifft Hetaryl-substituierte Guanidinverbindungen der allgemeinen Formel (I), die enantiomeren, diastereomeren und/oder tautomeren Formen davon sowie die pharmazeutisch annehmbaren Salze davon sowie die Prodrugs der genannten Verbindungen. Weiterhin betrifft die vorliegende Verbindung die Verwendung von Hetaryl-substituierten Guanidinverbindungen als Bindungspartner für 5-HT5-Rezeptoren zur Behandlung und/oder Prophylaxe von Krankheiten, die durch eine 5-HT5-Rezeptoraktivität moduliert werden, insbesondere zur Behandlung und/oder Prophylaxe von neurodegenerativen und neuropsychiatrischen Störungen sowie den damit zusammenhängenden Anzeichen, Symptomen und Fehlfunktionen.

Spiro-compounds as s1p modulators

The invention relates to heterocyclic compounds of formula (I) as SIP modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment or alleviation of diseases or disorders mediated by an SIP receptor.

Heterocyclic compounds, pharmaceutical compositions containing them, and their use as inhibitors of the glycine transporter 1

Heterocyclic carboxamides useful as inhibitors of phosphodiesterase type 10a

Disclosed are fused heterocyclic carboxamide compounds of formula (I) that are inhibitors of phosphodiesterase type 10A, wherein the variables are as defined in the specification. These inhibitors of phosphodiesterase type 10A are used for the manufacture of a medicament for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

Novel inhibitor compounds of phosphodiesterase type 10a

The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders wherein Y 1 and Y 2 are adjacent atoms in Het 1 , which are independently selected from the group consisting of carbon and nitrogen; k is 0, 1, 2 or 3; Het 1 is a bivalent monocyclic 5- or 6-membered heteroaromatic radical, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N-R a as ring members, or a bivalent fused bicyclic 8-, 9- or 10-membered heteroaromatic radical, having 1, 2, 3 or 4 heteroatoms or heteroatom moieties selected from O, S, N and N-R a as ring members; Het 2 is inter alia monocyclic 5- or 6-membered hetaryl, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N-R 1a as ring members, Cyc is inter alia optionally substituted monocyclic 5- or 6-membered hetaryl or optionally substituted fused 8-, 9- or 10-membered bicyclic hetaryl; Ar is optionally substituted phenylene or optionally substituted bivalent 6-membered hetaryl; R is attached to a carbon atom of Het 1 and inter alia - halogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -alkoxy, C 1 -C 6 -fluoroalkyl, C 1 -C 6 -fluoroalkoxy, C 3 -C 6 -cycloalkyl etc.

磷酸二酯酶第１０ａ型之新穎抑制劑化合物

本發明係關於作為磷酸二酯酶第10A型之抑制劑的式I化合物及其鹽等以及其用於製造藥物之用途，且因此該等化合物適用於治療或控制選自神經病症及精神病症之醫學病症，適用於改善與該等病症有關之症狀及適用於降低該等病症之風險。□其中Y1及Y2為Het1中之相鄰原子，其獨立地選自由碳及氮組成之群；k為0、1、2或3；Het1為具有1、2或3個選自O、S、N及N-Ra之雜原子或雜原子部分作為環成員的二價單環5員或6員雜芳族基，或具有1、2、3或4個選自O、S、N及N-Ra之雜原子或雜原子部分作為環成員的二價稠合雙環8員、9員或10員雜芳族基；Het2尤其為具有1、2或3個選自O、S、N及N-R1a之雜原子或雜原子部分作為環成員的單環5員或6員雜芳基，Cyc尤其為視情況經取代之單環5員或6員雜芳基或視情況經取代之稠合8員、9員或10員雙環雜芳基；Ar為視情況經取代之伸苯基或視情況經取代之二價6員雜芳基；R連接於Het1之碳原子且尤其為鹵素、C1-C6烷基、C2-C6烯基、C2-C6炔基、C1-C6烷氧基、C1-C6氟烷基、C1-C6氟烷氧基、C3-C6環烷基等。

Novel inhibitor compounds of phosphodiesterase type 10a

Compuestos inhibidores novedosos de fosfodiesterasa tipo 10a.

La presente invención se refiere a compuestos de la fórmula I y sus sales etc. que son inhibidores de fosfodiesterasa tipo 10A y a su uso para la fabricación de un medicamento y que por lo tanto son adecuados para tratar o controlar trastornos médicos seleccionados de trastornos neurológicos y trastornos psiquiátricos, para mejorar los síntomas asociados con tales trastornos y para reducir el riesgo de tales trastornos en donde Y1 e Y2 son átomos adyacentes en Het1, que se seleccionan independientemente del grupo que consiste de carbono y nitrógeno; k es 0, 1, 2 o 3; Het1 es un radical heteroaromático de 5 o 6 miembros monocíclico bivalente, que tiene 1, 2 o 3 heteroátomos o porciones de heteroátomo seleccionados de O, S, N y N-Ra como miembros del anillo, o un radical heteroaromático de 8, 9 o 10 miembros bicíclico fusionado bivalente, que tiene 1, 2, 3 o 4 heteroátomos o porciones de heteroátomo seleccionados de O, S, N y N-Ra como miembros del anillo; Het2 es inter alia hetarilo de 5 o 6 miembros monocíclico, que tiene 1, 2 o 3 heteroátomos o porciones de heteroátomo seleccionado de O, S, N y N-R1a como miembros del anillo, Cyc es inter alia hetarilo de 5 o 6 miembros monocíclico opcionalmente substituido o hetarilo bicíclico de 8, 9 o 10 miembros fusionado opcionalmente substituido; Ar es fenileno opcionalmente substituido o hetarilo opcionalmente substituido de 6 miembros bivalente; R se enlaza a un átomo de carbono de Het1 e inter alia - halógeno, alquilo C1-C6, alquenilo C2-C6, alquinilo C2-C6, alcoxi C1-C6, fluoroalquilo C1-C6, fluoroalcoxi C1-C6, cicloalquilo C3-C6 etc. (ver Fórmula).

composto inibidor de fosfodiesterase tipo 10a

resumo “composto inibidor de fosfodiesterase tipo 10a” a presente invenção refere-se a compostos da fórmula i e seus sais, etc, que são inibidores da fosfodiesterase tipo 10a e a sua utilização para a fabricação de um medicamento e que, portanto, são adequados para o tratamento ou controle de distúrbios médicos selecionados a partir de distúrbios neurológicos e distúrbios psiquiátricos, para melhorar os sintomas associados com tais distúrbios e para redu-zir o risco de tais distúrbios, em que y1 e y2 são átomos adjacentes em het1, os quais são independentemente selecionados a partir do grupo que consiste em car-bono e nitrogênio; k é 0, 1, 2 ou 3; het1 é um radical heteroaromático, com 5 ou 6 membros, monocíclico, bivalente, com 1, 2 ou 3 heteroátomos ou porções de hete-roátomos selecionados a partir de o, s, n e n-ra como membros do anel, ou um radical heteroaromático com 8, 9 ou 10 membros, bicíclico, fundido, bivalente, pos-suindo 1, 2, 3 ou 4 heteroátomos ou porções de heteroátomos selecionados a partir de o, s, n e n-ra como membros do anel; het2 é, inter alia, hetarila com 5 ou 6 membros, monocíclico possuindo 1, 2 ou 3 heteroátomos ou porções de heteroáto-mos selecionados a partir de o, s, n e n-r1a como membros do anel, cyc é, inter alia, hetarila com 5 ou 6 membros, monocíclico, opcionalmente substituído ou hetarila com 8, 9 ou 10 membros, bicíclico, fundido, opcionalmente substituído; ar é fenileno opcionalmente substituído ou hetarilacom 6 membros, bivalente, opcionalmente substituído; r está ligado a um átomo de carbono de het1 e, inter alia, - halogênio, c1-c6-alquila, c2-c6-alquenila, c2-c6-alquinila, c1-c6-alcóxi, c1-c6, fluoralquila, c1-c6-fluoralcóxi, c3-c6-cicloalquila, etc.

Verfahen zur herstellung von isocyanatgruppen und urethangruppen enthaltenden prepolymeren

Spiro-cyclic amine derivatives as s1p modulators

The present invention is directed to spiro-cyclic amine derivatives which are modulators of S1P receptors and are useful in the treatment of CNS disorders.

Verfahren zur herstellung von isocyanaten

Verfahren zur herstellung von isocyanaten

磷酸二酯酶第１０ａ型之新穎抑制劑化合物

本發明係關於式I化合物、其N-氧化物、互變異構體、前藥及醫藥上可接受的鹽。□其中，在式I中，變數R1、R2、R3、R4及R5係如技術方案中所定義，且其中X為C-R6或N，Y為C-R7或N，其中R6及R7尤其為氫、鹵素、烷氧基、鹵代烷氧基及類似基團。該等式I化合物、其N-氧化物、互變異構體、前藥及醫藥上可接受的鹽係磷酸二酯酶第10A型之抑制劑，且本發明係關於其等用於製造藥劑之用途，及因此該等物質適用於治療或控制選自神經疾病及精神疾病之醫學病症、舒緩與此等病症相關的症狀及降低此等病症之風險。